Entecavir monohydrate (Synonyms: 恩替卡韦 (1水合物); BMS200475 monohydrate; SQ34676 monohydrate)

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Entecavir monohydrate (BMS200475 monohydrate; SQ34676 monohydrate) 是有选择且有效地HBV抑制剂。在HepG2细胞中的EC₅₀值为3.75 nM。

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Entecavir monohydrate Chemical Structure

CAS No. : 209216-23-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥715	In-stock
1 mg	￥295	In-stock
5 mg	￥650	In-stock
10 mg	￥790	In-stock
50 mg	￥2068	In-stock
100 mg	￥3000	In-stock
200 mg	￥4800	In-stock
500 mg		询价
1 g		询价

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Other Forms of Entecavir monohydrate:

Entecavir In-stock
Entecavir monohydrate (Standard) 询价

MCE 顾客使用本产品发表的 19 篇科研文献

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Entecavir monohydrate (BMS200475 monohydrate; SQ34676 monohydrate) is a potent and selective inhibitor of HBV, with an EC₅₀ of 3.75 nM in HepG2 cell.

IC₅₀ & Target

EC50：3.75 nM (anti-HBV, HepG2 cell)^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CCRF-CEM	CC₅₀	> 100 μM Compound: Entecavir	Cytotoxicity against human CEM cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human CEM cells assessed as reduction in cell viability by MTT assay	[PMID: 33421915]
CEM-SS	CC₅₀	21 μM Compound: 4	Tested for cytotoxic concentration against human immunodeficiency virus (HIV) in CEM-SS cells Tested for cytotoxic concentration against human immunodeficiency virus (HIV) in CEM-SS cells	10.1016/S0960-894X(96)00594-X
CEM-SS	EC₅₀	21 μM Compound: ETV	Cytotoxicity against human CEM-SS cells after 10 days by MTT assay Cytotoxicity against human CEM-SS cells after 10 days by MTT assay	[PMID: 18316521]
CEM-SS	EC₅₀	> 10 μM Compound: 4	Tested for effective concentration to inhibit human immunodeficiency virus (HIV) in CEM-SS cells Tested for effective concentration to inhibit human immunodeficiency virus (HIV) in CEM-SS cells	10.1016/S0960-894X(96)00594-X
CEM-SS	EC₅₀	> 10 μM Compound: ETV	Antiviral activity against HIV1 infected in human CEM-SS cells after 10 days by MTT assay Antiviral activity against HIV1 infected in human CEM-SS cells after 10 days by MTT assay	[PMID: 18316521]
HEK293	EC₅₀	11.7 μM Compound: Entecavir	Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C/G190A mutant infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C/G190A mutant infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	12.5 μM Compound: Entecavir	Antiviral activity against HIV1 subtype A isolate 1 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype A isolate 1 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	12.6 μM Compound: Entecavir	Antiviral activity against HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	13.2 μM Compound: Entecavir	Antiviral activity against HIV1 subtype A isolate 2 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype A isolate 2 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	13.5 μM Compound: Entecavir	Antiviral activity against HIV1 subtype B isolate 4 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype B isolate 4 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	13.6 μM Compound: Entecavir	Antiviral activity against HIV1 subtype BF isolate 5 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype BF isolate 5 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	15.1 μM Compound: Entecavir	Antiviral activity against HIV1 subtype B isolate 3 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype B isolate 3 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	30.6 μM Compound: ETV	Antiviral activity against pseudotype HIV1 NL-Luc infected in 24 hrs pretreated HEK293 cells by phenosense assay Antiviral activity against pseudotype HIV1 NL-Luc infected in 24 hrs pretreated HEK293 cells by phenosense assay	[PMID: 18316521]
HEK293	EC₅₀	7.62 μM Compound: Entecavir	Antiviral activity against HIV1 subtype D isolate 8 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype D isolate 8 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	9.51 μM Compound: Entecavir	Antiviral activity against HIV1 subtype C isolate 6 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype C isolate 6 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	9.95 μM Compound: Entecavir	Antiviral activity against HIV1 subtype C isolate 7 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype C isolate 7 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	> 100 μM Compound: Entecavir	Antiviral activity against HIV1 expressing reverse transcriptase D67N/K70R/T215F/K219E/M184V mutant infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 expressing reverse transcriptase D67N/K70R/T215F/K219E/M184V mutant infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HFF	EC₅₀	15 μM Compound: 4	Tested for effective concentration required to inhibit human cytomegalovirus (HCMV) in HFF cells Tested for effective concentration required to inhibit human cytomegalovirus (HCMV) in HFF cells	10.1016/S0960-894X(96)00594-X
HeLa	EC₅₀	> 4 μM Compound: ETV	Antiviral activity against pseudotype HIV1 LAI-Luc infected in CD4-positive human HeLa cells measured on day 3 postinfection by luciferase reporter gene assay Antiviral activity against pseudotype HIV1 LAI-Luc infected in CD4-positive human HeLa cells measured on day 3 postinfection by luciferase reporter gene assay	[PMID: 18316521]
HepG2	CC₅₀	30 μM Compound: 4	Tested for the cytotoxicity against hepatitis B virus (HBV) in HepG2.2.15 cells Tested for the cytotoxicity against hepatitis B virus (HBV) in HepG2.2.15 cells	10.1016/S0960-894X(96)00594-X
HepG2	CC₅₀	42.07 μM Compound: ETV	Cytotoxicity in human HepG2 cells assessed as induction of cell killing Cytotoxicity in human HepG2 cells assessed as induction of cell killing	[PMID: 32421339]
HepG2	CC₅₀	> 100 μM Compound: Entecavir	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay	[PMID: 33421915]
HepG2	EC₅₀	0.003 μM Compound: 4	Tested for the effective concentration required to inhibit HBV in HepG2.2.15 human liver cells Tested for the effective concentration required to inhibit HBV in HepG2.2.15 human liver cells	10.1016/S0960-894X(96)00594-X
HepG2	EC₅₀	10.2 nM Compound: ETV	Inhibition of HBV replication with RT A200V substitution and L180M, M204I background from Lamivudine refractory patient transfected into HepG2 cells Inhibition of HBV replication with RT A200V substitution and L180M, M204I background from Lamivudine refractory patient transfected into HepG2 cells	[PMID: 17178796]
HepG2	EC₅₀	11 nM Compound: ETV	Inhibition of HBV replication with RT L80V substitution and L180M, M204V background from Lamivudine refractory patient transfected into HepG2 cells Inhibition of HBV replication with RT L80V substitution and L180M, M204V background from Lamivudine refractory patient transfected into HepG2 cells	[PMID: 17178796]
HepG2	EC₅₀	14.2 nM Compound: ETV	Inhibition of HBV replication with RT A181T substitution and V173L, L180M, M204V background from Lamivudine refractory patient transfected into HepG2 cells Inhibition of HBV replication with RT A181T substitution and V173L, L180M, M204V background from Lamivudine refractory patient transfected into HepG2 cells	[PMID: 17178796]
HepG2	EC₅₀	2.4 nM Compound: ETV	Inhibition of HBV replication with RT S78T substitution from Lamivudine refractory patient transfected into HepG2 cells Inhibition of HBV replication with RT S78T substitution from Lamivudine refractory patient transfected into HepG2 cells	[PMID: 17178796]
HepG2	EC₅₀	22.3 nM Compound: ETV	Inhibition of HBV replication with RT I53F substitution and V173F, L180M, M204V background from Lamivudine refractory patient transfected into HepG2 cells Inhibition of HBV replication with RT I53F substitution and V173F, L180M, M204V background from Lamivudine refractory patient transfected into HepG2 cells	[PMID: 17178796]
HepG2	EC₅₀	31.2 nM Compound: ETV	Inhibition of HBV replication with RT C188S substitution and L80I, L180T, M204V background from Lamivudine refractory patient transfected into HepG2 cells Inhibition of HBV replication with RT C188S substitution and L80I, L180T, M204V background from Lamivudine refractory patient transfected into HepG2 cells	[PMID: 17178796]
HepG2	EC₅₀	32.9 nM Compound: ETV	Inhibition of HBV replication with RT L229W substitution and L180M, M204V background from Lamivudine refractory patient transfected into HepG2 cells Inhibition of HBV replication with RT L229W substitution and L180M, M204V background from Lamivudine refractory patient transfected into HepG2 cells	[PMID: 17178796]
HepG2	EC₅₀	33 nM Compound: ETV	Inhibition of HBV replication with RT A200V substitution and M204I background from Lamivudine refractory patient transfected into HepG2 cells Inhibition of HBV replication with RT A200V substitution and M204I background from Lamivudine refractory patient transfected into HepG2 cells	[PMID: 17178796]
HepG2	EC₅₀	4 nM Compound: ETV	Inhibition of HBV replication with RT M309L substitution from Lamivudine refractory patient transfected into HepG2 cells Inhibition of HBV replication with RT M309L substitution from Lamivudine refractory patient transfected into HepG2 cells	[PMID: 17178796]
HepG2	EC₅₀	45.3 nM Compound: ETV	Inhibition of HBV replication with RT L80I substitution and L180M, M204I background from Lamivudine refractory patient transfected into HepG2 cells Inhibition of HBV replication with RT L80I substitution and L180M, M204I background from Lamivudine refractory patient transfected into HepG2 cells	[PMID: 17178796]
HepG2	EC₅₀	5.8 nM Compound: ETV	Inhibition of HBV replication with RT D263G substitution from Lamivudine refractory patient transfected into HepG2 cells Inhibition of HBV replication with RT D263G substitution from Lamivudine refractory patient transfected into HepG2 cells	[PMID: 17178796]
HepG2	EC₅₀	7.6 nM Compound: ETV	Inhibition of HBV replication with RT A200V substitution from Lamivudine refractory patient transfected into HepG2 cells Inhibition of HBV replication with RT A200V substitution from Lamivudine refractory patient transfected into HepG2 cells	[PMID: 17178796]
HepG2 2.2.15	CC₅₀	28 μM Compound: Entecavir	Cytotoxicity against human HepG2(2.2.15) cells after 24 hrs by neutral red dye uptake assay Cytotoxicity against human HepG2(2.2.15) cells after 24 hrs by neutral red dye uptake assay	[PMID: 21930377]
HepG2 2.2.15	CC₅₀	30 μM Compound: ETV	Cytotoxicity against human HepG2.2.15 cells by MTT assay Cytotoxicity against human HepG2.2.15 cells by MTT assay	[PMID: 25905540]
HepG2 2.2.15	CC₅₀	30 μM Compound: Entecavir	Cytotoxicity in human HepG2.215 cells assessed as reduction in cell viability after 5 days by CCK8 assay Cytotoxicity in human HepG2.215 cells assessed as reduction in cell viability after 5 days by CCK8 assay	[PMID: 28082068]
HepG2 2.2.15	CC₅₀	52.9 μM Compound: Entecavir	Cytotoxicity against human HepG2.2.15 cells after 7 days by MTT assay Cytotoxicity against human HepG2.2.15 cells after 7 days by MTT assay	[PMID: 30613328]
HepG2 2.2.15	CC₅₀	> 1 μM Compound: Entecavir	Cytotoxicity against human HepG2.2.15 cells assessed as cell viability by tetrazolium dye uptake assay Cytotoxicity against human HepG2.2.15 cells assessed as cell viability by tetrazolium dye uptake assay	[PMID: 28682067]
HepG2 2.2.15	EC₅₀	0.008 μM Compound: Entecavir	Antiviral activity against wild type Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot hybridization method Antiviral activity against wild type Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot hybridization method	[PMID: 21930377]
HepG2 2.2.15	EC₅₀	1.2 μM Compound: Entecavir	Antiviral activity against lamivudine/entecavir-resistant Hepatitis B virus harboring reverse transcriptase L180M/M204V/S202G infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot hybridization method Antiviral activity against lamivudine/entecavir-resistant Hepatitis B virus harboring reverse transcriptase L180M/M204V/S202G infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot hybridization method	[PMID: 21930377]
HepG2 2.2.15	EC₅₀	2.2 x 10^-6 μM Compound: ETV	Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in viral DNA levels incubated for 6 days by PCR analysis Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in viral DNA levels incubated for 6 days by PCR analysis	[PMID: 32421339]
Huh-7	CC₅₀	125 μM Compound: entecavir, ETV	Effect on cell viability in human Huh7 cells Effect on cell viability in human Huh7 cells	[PMID: 17371827]
Huh-7	CC₅₀	28 μM Compound: Entecavir	Cytotoxicity against human HuH7 cells Cytotoxicity against human HuH7 cells	[PMID: 23237841]
Huh-7	EC₅₀	0.008 μM Compound: Entecavir	Antiviral activity against wild type Hepatitis B virus infected in human HuH7 cells Antiviral activity against wild type Hepatitis B virus infected in human HuH7 cells	[PMID: 23237841]
Huh-7	EC₅₀	0.3 μM Compound: entecavir, ETV	Inhibition of wild type HBV replication in Huh7 cells Inhibition of wild type HBV replication in Huh7 cells	[PMID: 17371827]
Huh-7	EC₅₀	1.2 μM Compound: Entecavir	Antiviral activity against entecavir-resistant Hepatitis B virus harboring L180M/M204V/S202G triple mutant infected in human HuH7 cells Antiviral activity against entecavir-resistant Hepatitis B virus harboring L180M/M204V/S202G triple mutant infected in human HuH7 cells	[PMID: 23237841]
MOLT-4	EC₅₀	> 38 μM Compound: ETV	Antiviral activity against HIV1 3B infected in MOLT-4/3B cells assessed as inhibition of mature virus release measured after 4 days of infection by RT assay Antiviral activity against HIV1 3B infected in MOLT-4/3B cells assessed as inhibition of mature virus release measured after 4 days of infection by RT assay	[PMID: 18316521]
MT2	EC₅₀	0.056 μM Compound: ETV	Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells	[PMID: 18316521]
MT2	EC₅₀	0.056 μM Compound: ETV	Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
MT2	EC₅₀	0.071 μM Compound: ETV	Antiviral activity against HIV1 subtype B-LAI infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA Antiviral activity against HIV1 subtype B-LAI infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA	[PMID: 18316521]
MT2	EC₅₀	0.081 μM Compound: ETV	Antiviral activity against HIV1 subtype B-3B infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA Antiviral activity against HIV1 subtype B-3B infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA	[PMID: 18316521]
MT2	EC₅₀	0.085 μM Compound: ETV	Antiviral activity against HIV1 subtype B-NL4-3 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA Antiviral activity against HIV1 subtype B-NL4-3 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA	[PMID: 18316521]
MT2	EC₅₀	0.095 μM Compound: ETV	Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
MT2	EC₅₀	0.151 μM Compound: ETV	Antiviral activity against 0.006 MOI HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.006 MOI HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
MT2	EC₅₀	0.287 μM Compound: ETV	Antiviral activity against 0.006 MOI HIV1 NL4-3 infected in 1 hr-pretreated human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.006 MOI HIV1 NL4-3 infected in 1 hr-pretreated human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
MT2	EC₅₀	0.449 μM Compound: ETV	Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
MT2	EC₅₀	0.526 μM Compound: ETV	Antiviral activity against HIV1 subtype B-SF-2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA Antiviral activity against HIV1 subtype B-SF-2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA	[PMID: 18316521]
MT2	EC₅₀	0.839 μM Compound: ETV	Antiviral activity against HIV1 subtype B-RF infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA Antiviral activity against HIV1 subtype B-RF infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA	[PMID: 18316521]
MT2	EC₅₀	1.03 μM Compound: ETV	Antiviral activity against HIV1 subtype B-HXB2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA Antiviral activity against HIV1 subtype B-HXB2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA	[PMID: 18316521]
MT2	EC₅₀	1.3 μM Compound: ETV	Antiviral activity against pseudotype HIV1 NL-RLuc infected in human MT2 cells measured on day 5 postinfection by luciferase reporter gene assay Antiviral activity against pseudotype HIV1 NL-RLuc infected in human MT2 cells measured on day 5 postinfection by luciferase reporter gene assay	[PMID: 18316521]
MT2	EC₅₀	1.364 μM Compound: ETV	Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay	[PMID: 18316521]
MT2	EC₅₀	1.4 μM Compound: ETV	Antiviral activity against HIV1 subtype B-NL4-3 infected in 2 hrs pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA Antiviral activity against HIV1 subtype B-NL4-3 infected in 2 hrs pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA	[PMID: 18316521]
MT2	EC₅₀	13.5 μM Compound: ETV	Antiviral activity against 0.006 MOI HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.006 MOI HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
MT2	EC₅₀	3.62 μM Compound: ETV	Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
MT2	EC₅₀	30.6 μM Compound: ETV	Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells by phenosense assay Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells by phenosense assay	[PMID: 18316521]
MT2	EC₅₀	6.45 μM Compound: ETV	Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
MT2	EC₅₀	9.573 μM Compound: ETV	Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
MT2	EC₅₀	> 1.2 μM Compound: ETV	Antiviral activity against pseudotype HIV1 LAI-Luc infected in human MT2 cells measured on day 3 postinfection by luciferase reporter gene assay Antiviral activity against pseudotype HIV1 LAI-Luc infected in human MT2 cells measured on day 3 postinfection by luciferase reporter gene assay	[PMID: 18316521]
MT2	EC₅₀	> 10 μM Compound: ETV	Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring M184V mutant RT infected in human MT2 cells Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring M184V mutant RT infected in human MT2 cells	[PMID: 18316521]
MT2	EC₅₀	> 10 μM Compound: ETV	Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay	[PMID: 18316521]
MT2	EC₅₀	> 10 μM Compound: ETV	Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay	[PMID: 18316521]
MT2	EC₅₀	> 10 μM Compound: ETV	Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay	[PMID: 18316521]
MT2	EC₅₀	> 10 μM Compound: ETV	Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay	[PMID: 18316521]
MT2	EC₅₀	> 10 μM Compound: ETV	Antiviral activity against HIV1 NL4-3 harboring M184L mutant RT infected in human MT2 cellssmeasured after 7 passages on day 34 postinfection Antiviral activity against HIV1 NL4-3 harboring M184L mutant RT infected in human MT2 cellssmeasured after 7 passages on day 34 postinfection	[PMID: 18316521]
MT2	EC₅₀	> 10 μM Compound: ETV	Antiviral activity against HIV1 subtype B-NL4-3 infected in 3 hrs pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA Antiviral activity against HIV1 subtype B-NL4-3 infected in 3 hrs pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA	[PMID: 18316521]
MT2	EC₅₀	> 100 μM Compound: ETV	Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring M184V mutant RT infected in human MT2 cells by phenosense assay Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring M184V mutant RT infected in human MT2 cells by phenosense assay	[PMID: 18316521]
MT2	EC₅₀	> 10000 μM Compound: ETV	Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
MT2	EC₅₀	> 10000 μM Compound: ETV	Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
MT2	EC₅₀	> 2.901 μM Compound: ETV	Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay	[PMID: 18316521]
MT2	EC₅₀	> 6.348 μM Compound: ETV	Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay	[PMID: 18316521]
MT2	EC₅₀	> 9.693 μM Compound: ETV	Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay	[PMID: 18316521]
PBMC	CC₅₀	15.7 μM Compound: Entecavir	Cytotoxicity against human PBMC cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human PBMC cells assessed as reduction in cell viability by MTT assay	[PMID: 33421915]
PBMC	EC₅₀	0.026 μM Compound: ETV	Antiviral activity against HIV1 subtype B-ASM 044 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA Antiviral activity against HIV1 subtype B-ASM 044 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA	[PMID: 18316521]
PBMC	EC₅₀	0.062 μM Compound: ETV	Antiviral activity against HIV1 subtype B-92US076 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA Antiviral activity against HIV1 subtype B-92US076 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA	[PMID: 18316521]
PBMC	EC₅₀	0.109 μM Compound: ETV	Antiviral activity against HIV1 subtype B-ASM 034 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA Antiviral activity against HIV1 subtype B-ASM 034 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA	[PMID: 18316521]
PBMC	EC₅₀	1.753 μM Compound: ETV	Antiviral activity against HIV1 subtype B-93US143 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA Antiviral activity against HIV1 subtype B-93US143 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA	[PMID: 18316521]
Vero	CC₅₀	> 100 μM Compound: Entecavir	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability by MTT assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability by MTT assay	[PMID: 33421915]
WI-38	CC₅₀	120 μM Compound: 4	Tested for cytotoxic concentration against varicella zoster virus (VZV) in WI-38 cells Tested for cytotoxic concentration against varicella zoster virus (VZV) in WI-38 cells	10.1016/S0960-894X(96)00594-X
WI-38	CC₅₀	> 90 μM Compound: 4	Tested for cytotoxic concentration against herpes simplex virus type 1 (HSV-1) in WI-38 cells Tested for cytotoxic concentration against herpes simplex virus type 1 (HSV-1) in WI-38 cells	10.1016/S0960-894X(96)00594-X
WI-38	EC₅₀	30 μM Compound: 4	Tested for effective concentration required to inhibit varicella zoster virus (VZV) in WI-38 cells; 30-60 Tested for effective concentration required to inhibit varicella zoster virus (VZV) in WI-38 cells; 30-60	10.1016/S0960-894X(96)00594-X
WI-38	EC₅₀	>= 32 μM Compound: 4	Tested for effective concentration required to inhibit herpes simplex virus type 1 (HSV-1) in WI-38 cells Tested for effective concentration required to inhibit herpes simplex virus type 1 (HSV-1) in WI-38 cells	10.1016/S0960-894X(96)00594-X

体外研究
(In Vitro)

Entecavir monohydrate (BMS200475 monohydrate；SQ34676 monohydrate) 对 HBV 的 EC₅₀ 为 3.75 nM。它被整合到 HBV 的蛋白质引物中，随后抑制逆转录酶的启动步骤。BMS -200475 对其他 RNA 和 DNA 病毒的抗病毒活性明显较低^[1]。
与其他脱氧鸟苷类似物（Penciclovir, Ganciclovir, Lobucavir, 和 Aciclovir) 或 Iamivudine，Entecavir monohydrate 更容易磷酸化为其活性代谢物。Entecavir 的细胞内半衰期为 15 小时^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

每日口服 Entecavir (monohydrate)，剂量范围为 0.02-0.5 mg/kg，持续 1-3 个月，可有效降低慢性感染土拨鼠的土拨鼠肝炎病毒 (WHV) 病毒血症水平^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

295.29

Formula

C₁₂H₁₇N₅O₄

CAS 号

209216-23-9

性状

固体

颜色

White to off-white

中文名称

恩替卡韦 (1水合物)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 50 mg/mL (169.33 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : 2.8 mg/mL (9.48 mM; 超声加热助溶)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.3865 mL	16.9325 mL	33.8650 mL
5 mM	0.6773 mL	3.3865 mL	6.7730 mL
10 mM	0.3387 mL	1.6933 mL	3.3865 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (10.16 mM); 澄清溶液

此方案可获得 ≥ 3 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (10.16 mM); 澄清溶液

此方案可获得 ≥ 3 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 3 mg/mL (10.16 mM); 澄清溶液

此方案可获得 ≥ 3 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.85%

选择批次：

Data Sheet (646 KB) SDS (393 KB)

COA (291 KB) HNMR (168 KB) LCMS (94 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Innaimo SF, et al. Identification of?BMS-200475?as a potent and selective inhibitor of hepatitis B virus. Antimicrob Agents Chemother. 1997 Jul;41(7):1444-8. [Content Brief]

[2]. Rivkin A, et al. A review of entecavir in the treatment of chronic hepatitis B infection. Curr Med Res Opin.?2005 Nov;21(11):1845-56. [Content Brief]

[3]. Genovesi EV, et al. Efficacy of the carbocyclic 2'-deoxyguanosine nucleoside?BMS-200475?in the woodchuck model of hepatitis B virus infection. Antimicrob Agents Chemother.?1998 Dec;42(12):3209-17. [Content Brief]

Cell Assay ^[1]	BMS 200475 is prepared in phosphate-buffered saline (PBS) and diluted with appropriate medium containing 2% fetal bovine serum. HepG2 2.2.15 cells are plated at a density of 5×10⁵ cells per well on 12-well Biocoat collagen-coated plates and are maintained in a confluent state for 2 to 3 days before being overlaid with 1 mL of medium spiked with BMS 200475. Quantification of HBV was performed on day 10^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Innaimo SF, et al. Identification of?BMS-200475?as a potent and selective inhibitor of hepatitis B virus. Antimicrob Agents Chemother. 1997 Jul;41(7):1444-8. [Content Brief] [2]. Rivkin A, et al. A review of entecavir in the treatment of chronic hepatitis B infection. Curr Med Res Opin.?2005 Nov;21(11):1845-56. [Content Brief] [3]. Genovesi EV, et al. Efficacy of the carbocyclic 2'-deoxyguanosine nucleoside?BMS-200475?in the woodchuck model of hepatitis B virus infection. Antimicrob Agents Chemother.?1998 Dec;42(12):3209-17. [Content Brief]

Cell Assay
^[1]

BMS 200475 is prepared in phosphate-buffered saline (PBS) and diluted with appropriate medium containing 2% fetal bovine serum. HepG2 2.2.15 cells are plated at a density of 5×10⁵ cells per well on 12-well Biocoat collagen-coated plates and are maintained in a confluent state for 2 to 3 days before being overlaid with 1 mL of medium spiked with BMS 200475. Quantification of HBV was performed on day 10^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[1]. Innaimo SF, et al. Identification of?BMS-200475?as a potent and selective inhibitor of hepatitis B virus. Antimicrob Agents Chemother. 1997 Jul;41(7):1444-8. [Content Brief]

[2]. Rivkin A, et al. A review of entecavir in the treatment of chronic hepatitis B infection. Curr Med Res Opin.?2005 Nov;21(11):1845-56. [Content Brief]

[3]. Genovesi EV, et al. Efficacy of the carbocyclic 2'-deoxyguanosine nucleoside?BMS-200475?in the woodchuck model of hepatitis B virus infection. Antimicrob Agents Chemother.?1998 Dec;42(12):3209-17. [Content Brief]

Entecavir monohydrate 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	3.3865 mL	16.9325 mL	33.8650 mL	84.6625 mL
H₂O / DMSO	5 mM	0.6773 mL	3.3865 mL	6.7730 mL	16.9325 mL
DMSO	10 mM	0.3387 mL	1.6933 mL	3.3865 mL	8.4663 mL
	15 mM	0.2258 mL	1.1288 mL	2.2577 mL	5.6442 mL
	20 mM	0.1693 mL	0.8466 mL	1.6933 mL	4.2331 mL
	25 mM	0.1355 mL	0.6773 mL	1.3546 mL	3.3865 mL
	30 mM	0.1129 mL	0.5644 mL	1.1288 mL	2.8221 mL
	40 mM	0.0847 mL	0.4233 mL	0.8466 mL	2.1166 mL
	50 mM	0.0677 mL	0.3387 mL	0.6773 mL	1.6933 mL
	60 mM	0.0564 mL	0.2822 mL	0.5644 mL	1.4110 mL
	80 mM	0.0423 mL	0.2117 mL	0.4233 mL	1.0583 mL
	100 mM	0.0339 mL	0.1693 mL	0.3387 mL	0.8466 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Entecavir209216-23-9BMS200475SQ34676恩替卡韦 (1水合物)BMS 200475BMS-200475SQ 34676SQ-34676HBVHepatitis B virusInhibitorinhibitorinhibit

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Entecavir monohydrate (Synonyms: 恩替卡韦 (1水合物); BMS200475 monohydrate; SQ34676 monohydrate)

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Other Forms of Entecavir monohydrate:

MCE 顾客使用本产品发表的 19 篇科研文献

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稀释计算器

Entecavir monohydrate 相关分类

完整储备液配制表

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Entecavir monohydrate (Synonyms: 恩替卡韦 (1水合物); BMS200475 monohydrate; SQ34676 monohydrate)

Customer Review

Other Forms of Entecavir monohydrate:

Entecavir monohydrate 相关抗体

MCE 顾客使用本产品发表的 19 篇科研文献

Entecavir monohydrate 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

Entecavir monohydrate 相关抗体:

摩尔计算器

稀释计算器

Entecavir monohydrate 相关分类

完整储备液配制表

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