Oseltamivir acid (Synonyms: 奥斯他伟酸; GS 4071; Ro 64-0802; Oseltamivir carboxylate)

目录号: HY-13318 纯度: 99.50%: Data Sheet SDS COA 产品使用指南
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技术支持

Oseltamivir acid (GS 4071)，Oseltamivir phosphate 的活性代谢产物, 是流感病毒神经氨酸酶 (IC₅₀=2 nM) 的口服生物有效的，选择性的抑制剂，对流感病毒 A 和 B 都有活性。

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Oseltamivir acid Chemical Structure

CAS No. : 187227-45-8

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥715	In-stock
1 mg	￥285	In-stock
5 mg	￥650	In-stock
10 mg	￥1100	In-stock
25 mg	￥2310	In-stock
50 mg	￥3465	In-stock
100 mg	￥4950	In-stock
200 mg		询价
500 mg		询价

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Customer Review

Other Forms of Oseltamivir acid:

MCE 顾客使用本产品发表的 71 篇科研文献

Proliferation Assay

: Oseltamivir acid purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Jan:97:385-394. [Abstract]; The inhibitory effects of OA on M1 protein synthesis and in three different infection protocols. M1 protein expression in H1N1-infected MDCK cells analyzed by Western blot 24 h post infection.

: Oseltamivir acid purchased from MCE. Usage Cited in: Antiviral Res. 2016 May:129:81-92. [Abstract]; MDCK cells are infected with K435E or H274Y in the absence of compounds and maintained at 35 °C in agarose with or without 10 nM Oseltamivir or 20 μg/mL D35, respectively.

: Oseltamivir acid purchased from MCE. Usage Cited in: PLoS One. 2016 May 27;11(5):e0156400. [Abstract]; Live-cell fluorescence imaging of infected cells of Oseltamivir-resistant virus. MDCK cells are infected with Oseltamivir-resistant 738 and -sensitive 838. After incubation at 37°C for 12 hr, the cells are incubated with BTP3-Neu5Ac with or without Oseltamivir or Zanamivir (each 100 nM for final concentrations) in an SFM at 37°C for 10 min. Fluorescent images of the cells are observed under UV irradiation by using a fluorescence microscope. A scale bar indicates 200 μm.

: Oseltamivir acid purchased from MCE. Usage Cited in: Antiviral Res. 2014 Nov;111:69-77. [Abstract]; Plaque formation of different recombinant viruses in the presence of oseltamivir. MDCK cells are infected with recombinant viruses in the absence of Oseltamivir or DS and maintained in agarose overlay medium with 50 nM Oseltamivir or 100 μg/mL DS (DS), or without compounds (None) at 35 °C.

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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

Oseltamivir acid (GS 4071), the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC₅₀=2 nM) with activity against both influenza A and B viruses^[1]^[2].

IC₅₀ & Target

IC50: 2 nM (influenza virus neuraminidase)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	CC₅₀	61.2 μM Compound: OSC	Cytotoxicity against human A549 cells by SRB assay Cytotoxicity against human A549 cells by SRB assay	[PMID: 38608962]
Fibroblast	CC₅₀	> 100 μM Compound: OSC	Cytotoxicity against chicken embryo fibroblast cells assessed as reduction in cell growth by CCK-8 Cytotoxicity against chicken embryo fibroblast cells assessed as reduction in cell growth by CCK-8	[PMID: 37804770]
Fibroblast	CC₅₀	> 1000 μM Compound: OSC	Cytotoxicity against chicken embryo fibroblasts assessed as reduction in cell viability after 2 days by CCK-8 assay Cytotoxicity against chicken embryo fibroblasts assessed as reduction in cell viability after 2 days by CCK-8 assay	[PMID: 29407952]
Fibroblast	CC₅₀	> 200 μM Compound: 1; OSC	Cytotoxicity against chicken embryo fibroblasts after 48 hrs by CCK-8 assay Cytotoxicity against chicken embryo fibroblasts after 48 hrs by CCK-8 assay	[PMID: 29965752]
Fibroblast	CC₅₀	> 200 μM Compound: OSC	Cytotoxicity against chicken embryo fibroblasts assessed as reduction in cell viability after 48 hrs by CCK-8 assay Cytotoxicity against chicken embryo fibroblasts assessed as reduction in cell viability after 48 hrs by CCK-8 assay	[PMID: 30365885]
Fibroblast	CC₅₀	> 200 μM Compound: OSC	Cytotoxicity against chicken embryo fibroblast assessed as reduction in cell viability after 48 hrs by CCK8 assay Cytotoxicity against chicken embryo fibroblast assessed as reduction in cell viability after 48 hrs by CCK8 assay	[PMID: 32092589]
Fibroblast	CC₅₀	> 200 μM Compound: OSC	Cytotoxicity against chicken embryo fibroblast cells assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay Cytotoxicity against chicken embryo fibroblast cells assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 36931117]
Fibroblast	CC₅₀	> 250 μM Compound: OSC	Cytotoxicity against chick embryo fibroblast cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay Cytotoxicity against chick embryo fibroblast cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay	[PMID: 35939763]
Fibroblast	EC₅₀	12.32 μM Compound: OSC	Anti-influenza virus activity against Influenza A virus A/Goose/Guangdong/SH7/2013 (H5N1) infected in chicken embryo fibroblast assessed as protection against virus-induced cytopathic effect incubated for 48 hrs by CCK-8 assay Anti-influenza virus activity against Influenza A virus A/Goose/Guangdong/SH7/2013 (H5N1) infected in chicken embryo fibroblast assessed as protection against virus-induced cytopathic effect incubated for 48 hrs by CCK-8 assay	[PMID: 36931117]
Fibroblast	EC₅₀	2.96 μM Compound: OSC	Anti-influenza virus activity against Influenza A virus A/Goose/Jiangsu/1306/2014 (H5N8) infected in chicken embryo fibroblast assessed as protection against virus-induced cytopathic effect incubated for 48 hrs by CCK-8 assay Anti-influenza virus activity against Influenza A virus A/Goose/Jiangsu/1306/2014 (H5N8) infected in chicken embryo fibroblast assessed as protection against virus-induced cytopathic effect incubated for 48 hrs by CCK-8 assay	[PMID: 36931117]
HEK-293T	CC₅₀	> 250 μM Compound: OSV	Cytotoxicity against HEK293T cells assessed as decrease in cell viability after 24 hrs by MTT assay Cytotoxicity against HEK293T cells assessed as decrease in cell viability after 24 hrs by MTT assay	[PMID: 30142611]
HEK293	IC₅₀	0.4 nM Compound: 3a	Inhibition of oseltamivir-resistant Influenza A virus A/WSN/1933(H1N1) recombinant wild type neuraminidase transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measured after 15 mins by fluorometric assay Inhibition of oseltamivir-resistant Influenza A virus A/WSN/1933(H1N1) recombinant wild type neuraminidase transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measured after 15 mins by fluorometric assay	[PMID: 27167096]
HEK293	IC₅₀	0.6 nM Compound: 3a	Inhibition of Influenza A virus A/Brisbane/10/2007(H3N2) recombinant wild type neuraminidase transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measured after 15 mins by fluorometric assay Inhibition of Influenza A virus A/Brisbane/10/2007(H3N2) recombinant wild type neuraminidase transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measured after 15 mins by fluorometric assay	[PMID: 27167096]
HEK293	IC₅₀	0.9 nM Compound: 3a	Inhibition of oseltamivir-resistant Influenza A virus A/Vietnam/1194/2004(H5N1) recombinant wild type neuraminidase transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measured after 15 mins by fluorometric assay Inhibition of oseltamivir-resistant Influenza A virus A/Vietnam/1194/2004(H5N1) recombinant wild type neuraminidase transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measured after 15 mins by fluorometric assay	[PMID: 27167096]
HEK293	IC₅₀	1 nM Compound: 3a	Inhibition of Influenza A virus A/Shanghai/01/2014(H7N9) recombinant wild type neuraminidase transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measured after 15 mins by fluorometric assay Inhibition of Influenza A virus A/Shanghai/01/2014(H7N9) recombinant wild type neuraminidase transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measured after 15 mins by fluorometric assay	[PMID: 27167096]
HEK293	IC₅₀	26 nM Compound: 3a	Inhibition of oseltamivir-resistant Influenza A virus A/Vietnam/1194/2004(H5N1) recombinant neuraminidase H275Y mutant transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measured after 15 mins by fluorometric assay Inhibition of oseltamivir-resistant Influenza A virus A/Vietnam/1194/2004(H5N1) recombinant neuraminidase H275Y mutant transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measured after 15 mins by fluorometric assay	[PMID: 27167096]
HEK293	IC₅₀	4371 nM Compound: 3a	Inhibition of Influenza A virus A/Brisbane/10/2007(H3N2) recombinant neuraminidase R292K mutant transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measured after 15 mins by fluorometric assay Inhibition of Influenza A virus A/Brisbane/10/2007(H3N2) recombinant neuraminidase R292K mutant transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measured after 15 mins by fluorometric assay	[PMID: 27167096]
HEK293	IC₅₀	49 nM Compound: 3a	Inhibition of Influenza A virus A/WSN/1933(H1N1) recombinant neuraminidase H275Y mutant transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measured after 15 mins by fluorometric assay Inhibition of Influenza A virus A/WSN/1933(H1N1) recombinant neuraminidase H275Y mutant transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measured after 15 mins by fluorometric assay	[PMID: 27167096]
HEK293	IC₅₀	> 83000 nM Compound: 3a	Inhibition of Influenza A virus A/Brisbane/10/2007(H3N2) recombinant neuraminidase E119A mutant transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measured after 15 mins by fluorometric assay Inhibition of Influenza A virus A/Brisbane/10/2007(H3N2) recombinant neuraminidase E119A mutant transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measured after 15 mins by fluorometric assay	[PMID: 27167096]
HeLa	CC₅₀	> 1000 μM Compound: B	Cytotoxicity against human HeLa cells measured at 24 hrs post dose Cytotoxicity against human HeLa cells measured at 24 hrs post dose	[PMID: 28182988]
HeLa	CC₅₀	> 1000 μM Compound: B	Cytotoxicity against human HeLa cells measured at 48 hrs post dose Cytotoxicity against human HeLa cells measured at 48 hrs post dose	[PMID: 28182988]
MDCK	CC₅₀	17.12 μM Compound: Oseltamivir carboxylic acid	Cytotoxicity against MDCK cells by MTT assay Cytotoxicity against MDCK cells by MTT assay	[PMID: 18640042]
MDCK	CC₅₀	250 μM Compound: OSC	Cytotoxicity against dog MDCK cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay Cytotoxicity against dog MDCK cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay	[PMID: 34735766]
MDCK	CC₅₀	66 μM Compound: Oseltamivir carboxylate	Cytotoxicity against MDCK cells Cytotoxicity against MDCK cells	[PMID: 32360104]
MDCK	CC₅₀	713.4 μM Compound: OMVA	Cytotoxicity against dog MDCK cells assessed as reduction in cell viability by MTT assay Cytotoxicity against dog MDCK cells assessed as reduction in cell viability by MTT assay	[PMID: 31744778]
MDCK	CC₅₀	> 100 μM Compound: 2b; OC	Cytotoxicity against MDCK cells after 48 hrs by CellTiter96 aqueous non-radioactive cell proliferation assay Cytotoxicity against MDCK cells after 48 hrs by CellTiter96 aqueous non-radioactive cell proliferation assay	[PMID: 29843102]
MDCK	CC₅₀	> 100 μM Compound: OC	Cytotoxicity against MDCK cells assessed as reduction in cell viability measured after 72 hrs by CCK8 analysis Cytotoxicity against MDCK cells assessed as reduction in cell viability measured after 72 hrs by CCK8 analysis	[PMID: 34839161]
MDCK	CC₅₀	> 100 μM Compound: Oseltamivir carboxylate	Cytotoxicity against MDCK cells assessed as cell viability measured after 4 days by formazan-based MTS assay Cytotoxicity against MDCK cells assessed as cell viability measured after 4 days by formazan-based MTS assay	[PMID: 27112451]
MDCK	CC₅₀	> 100 μM Compound: Oseltamivir carboxylate	Cytotoxicity in dog MDCK cells assessed as reduction in cell viability measured after 3 days by beckman coulter counting method Cytotoxicity in dog MDCK cells assessed as reduction in cell viability measured after 3 days by beckman coulter counting method	[PMID: 33894564]
MDCK	CC₅₀	> 100 μM Compound: Oseltamivir carboxylate	Cytotoxicity against MDCK cells infected with Influenza A virus A/Anhui/1/2013 (H7N9) assessed as reduction in cell viability Cytotoxicity against MDCK cells infected with Influenza A virus A/Anhui/1/2013 (H7N9) assessed as reduction in cell viability	[PMID: 34808389]
MDCK	CC₅₀	> 100 μM Compound: Oseltamivir carboxylate	Cytotoxicity against MDCK cells infected with Influenza A virus A/Puerto Rico/8/34 (H1N1) assessed as reduction in cell viability Cytotoxicity against MDCK cells infected with Influenza A virus A/Puerto Rico/8/34 (H1N1) assessed as reduction in cell viability	[PMID: 34808389]
MDCK	CC₅₀	> 1000 μM Compound: 5; OC	Cytotoxicity against dog MDCK cells assessed as reduction in cell viability incubated for 72 hrs by celltiterglo reagent based assay Cytotoxicity against dog MDCK cells assessed as reduction in cell viability incubated for 72 hrs by celltiterglo reagent based assay	[PMID: 31708183]
MDCK	CC₅₀	> 1000 μM Compound: B	Cytotoxicity against MDCK cells measured at 24 hrs post dose Cytotoxicity against MDCK cells measured at 24 hrs post dose	[PMID: 28182988]
MDCK	CC₅₀	> 1000 μM Compound: B	Cytotoxicity against MDCK cells measured at 48 hrs post dose Cytotoxicity against MDCK cells measured at 48 hrs post dose	[PMID: 28182988]
MDCK	CC₅₀	> 1 x 10⁵ nM Compound: 3a	Cytotoxicity against MDCK cells after 48 hrs by CellTiter 96 AQueous Non-Radioactive cell proliferation assay Cytotoxicity against MDCK cells after 48 hrs by CellTiter 96 AQueous Non-Radioactive cell proliferation assay	[PMID: 27167096]
MDCK	CC₅₀	> 20 μM Compound: Oseltamivir carboxylate	Cytotoxicity against MDCK cells after 48 hrs by neutral red uptake assay Cytotoxicity against MDCK cells after 48 hrs by neutral red uptake assay	[PMID: 30429954]
MDCK	CC₅₀	> 250 μM Compound: 1; OSC	Cytotoxicity against MDCK cells after 48 hrs by MTT assay Cytotoxicity against MDCK cells after 48 hrs by MTT assay	[PMID: 29965752]
MDCK	CC₅₀	> 250 μM Compound: OSC	Cytotoxicity against MDCK cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against MDCK cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 30365885]
MDCK	CC₅₀	> 250 μM Compound: OSC	Cytotoxicity against MDCK cells assessed as reduction in cell viability by MTT assay Cytotoxicity against MDCK cells assessed as reduction in cell viability by MTT assay	[PMID: 33385836]
MDCK	CC₅₀	> 250 μM Compound: OSC	Cytotoxicity against MDCK cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against MDCK cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 35939763]
MDCK	CC₅₀	> 250 μM Compound: OSC	Cytotoxicity against dog MDCK cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay Cytotoxicity against dog MDCK cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay	[PMID: 36931117]
MDCK	CC₅₀	> 250 μM Compound: OSV	Cytotoxicity against MDCK cells assessed as decrease in cell viability after 48 hrs by MTT assay Cytotoxicity against MDCK cells assessed as decrease in cell viability after 48 hrs by MTT assay	[PMID: 30142611]
MDCK	CC₅₀	> 30 μg/mL Compound: Oseltamivir carboxylate	Cytotoxicity in MDCK cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in MDCK cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31375291]
MDCK	EC₅₀	1.4 μM Compound: Oseltamivir carboxylate	Antiviral activity against Influenza A virus A/PR/8/34 infected in MDCK cells assessed as reduction of virus-induced cytopathic effect measured after 4 days by formazan-based MTS assay Antiviral activity against Influenza A virus A/PR/8/34 infected in MDCK cells assessed as reduction of virus-induced cytopathic effect measured after 4 days by formazan-based MTS assay	[PMID: 27112451]
MDCK	EC₅₀	11026 nM Compound: 1a, OC	Antiviral activity against Influenza A virus A/WSN/1933(H1N1) harboring neuraminidase H275Y mutant infected in MDCK cells assessed as virus-mediated cytopathic effect after 48 hrs by CellTiter96 assay Antiviral activity against Influenza A virus A/WSN/1933(H1N1) harboring neuraminidase H275Y mutant infected in MDCK cells assessed as virus-mediated cytopathic effect after 48 hrs by CellTiter96 assay	[PMID: 25456388]
MDCK	EC₅₀	28.2 nM Compound: 1a, OC	Antiviral activity against Influenza A virus A/WSN/1933(H1N1) infected in MDCK cells assessed as virus-mediated cytopathic effect after 48 hrs by CellTiter96 assay Antiviral activity against Influenza A virus A/WSN/1933(H1N1) infected in MDCK cells assessed as virus-mediated cytopathic effect after 48 hrs by CellTiter96 assay	[PMID: 25456388]
MDCK	EC₅₀	4 μM Compound: Oseltamivir carboxylate	Antiviral activity against Influenza A virus A/PR/8/34 infected in MDCK cells assessed as reduction of virus induced cytopathic effect measured by visual scoring of cytopathic effect Antiviral activity against Influenza A virus A/PR/8/34 infected in MDCK cells assessed as reduction of virus induced cytopathic effect measured by visual scoring of cytopathic effect	[PMID: 27112451]
MDCK	EC₅₀	5.21 μM Compound: 5	Antiviral activity against Influenza A virus A/Jena/5258/2009(H1N1) infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect after 48 hrs Antiviral activity against Influenza A virus A/Jena/5258/2009(H1N1) infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect after 48 hrs	[PMID: 24422530]
MDCK	EC₅₀	5.5 nM Compound: 3a	Antiviral activity against oseltamivir-resistant Influenza A virus A/WSN/1933(H1N1) infected in MDCK cells assessed as protection against virus-induced cytopathic effect after 48 hrs by CellTiter 96 AQueous Non-Radioactive cell proliferation assay Antiviral activity against oseltamivir-resistant Influenza A virus A/WSN/1933(H1N1) infected in MDCK cells assessed as protection against virus-induced cytopathic effect after 48 hrs by CellTiter 96 AQueous Non-Radioactive cell proliferation assay	[PMID: 27167096]
MDCK	EC₅₀	7.1 nM Compound: OMVA	Antiviral activity against Influenza A virus (H1N1) infected in dog MDCK cells assessed as reduction in log2HA titer incubated for 3 to 4 days by CPE assay Antiviral activity against Influenza A virus (H1N1) infected in dog MDCK cells assessed as reduction in log2HA titer incubated for 3 to 4 days by CPE assay	[PMID: 31744778]
MDCK	EC₅₀	> 100 μM Compound: 5	Antiviral activity against Oseltamivir-resistant Influenza A virus A/Berlin/55/08(H1N1) infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect after 48 hrs Antiviral activity against Oseltamivir-resistant Influenza A virus A/Berlin/55/08(H1N1) infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect after 48 hrs	[PMID: 24422530]
MDCK	IC₅₀	13 μM Compound: Oseltamivir carboxylate	Inhibition of M2 proton channel in Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in MDCK cells assessed as inhibition of viral infection Inhibition of M2 proton channel in Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in MDCK cells assessed as inhibition of viral infection	[PMID: 32360104]
Vero	CC₅₀	> 1000 μM Compound: B	Cytotoxicity against African green monkey Vero cells measured at 24 hrs post dose Cytotoxicity against African green monkey Vero cells measured at 24 hrs post dose	[PMID: 28182988]
Vero	CC₅₀	> 1000 μM Compound: B	Cytotoxicity against African green monkey Vero cells measured at 48 hrs post dose Cytotoxicity against African green monkey Vero cells measured at 48 hrs post dose	[PMID: 28182988]

体外研究
(In Vitro)

Oseltamivir acid 在体外和体内抑制病毒复制。B 型和 A/H1N1 型流感病毒似乎对奥司他韦敏感 (平均 B IC₅₀ 值：13 nM；平均 H1N1 IC₅₀ 值：1.34 nM)，而 A/H1N2 和 A/H3N2 病毒对奥司他韦更敏感 (平均 H3N2 IC₅₀ 值：0.67 nM；平均 H1N2 IC₅₀ 值：0.9 nM)^[3]。
在甲型流感病毒的神经氨酸酶抑制试验中，RWJ-270201 的 IC₅₀ (约 0.34 nM) 与 Oseltamivir acid (0.45 nM) 相当。B 病毒分离株，RWJ-270201 (1.36 nM) 的 IC₅₀ 与 Zanamivir (2.7 nM) 相当，低于 Oseltamivir carboxylate (8.5 nM)^[4]。

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

体内研究
(In Vivo)

Oseltamivir acid (0.1、1 或 10 mg/kg/天，每日两次，口服强饲法) 对 Vietnam/1203/04 (VN1203/04) 病毒产生剂量依赖性抗病毒作用。10 mg/kg/天的 5 天方案可保护 50% 的小鼠；该处理组的死亡是延迟的，表明处理完成后残留病毒的复制。1 和 10 mg/kg/天的剂量显著降低了器官中的病毒滴度，并分别提供了 60% 和 80% 的存活率^[5]。

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

分子量

284.35

Formula

C₁₄H₂₄N₂O₄

CAS 号

187227-45-8

性状

固体

颜色

White to off-white

中文名称

奥斯他伟酸

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据

细胞实验：

H₂O 中的溶解度 : 250 mg/mL (879.20 mM; 超声助溶)

DMSO 中的溶解度 : ≥ 230 mg/mL (808.86 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)

* "≥" 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	3.5168 mL	17.5840 mL	35.1679 mL
5 mM	0.7034 mL	3.5168 mL	7.0336 mL
10 mM	0.3517 mL	1.7584 mL	3.5168 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, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 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: ≥ 5.75 mg/mL (20.22 mM); 澄清溶液

此方案可获得 ≥ 5.75 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 57.5 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: ≥ 5.75 mg/mL (20.22 mM); 澄清溶液

此方案可获得 ≥ 5.75 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 57.5 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: ≥ 5.75 mg/mL (20.22 mM); 澄清溶液

此方案可获得 ≥ 5.75 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 57.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。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： PBS
Solubility: 100 mg/mL (351.68 mM); 澄清溶液; 超声助溶

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

计算结果

工作液所需浓度 : mg/mL

该产品水溶性佳，请具体参考实测水 / PBS / Saline 中的溶解度数据。

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

纯度 & 产品资料

纯度: 99.80%

选择批次：

Data Sheet (650 KB) SDS (393 KB)

COA (288 KB) LCMS (90 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Li W, et al. Identification of GS 4104 as an orally bioavailable prodrug of the influenza virus neuraminidase inhibitor GS 4071. Antimicrob Agents Chemother. 1998 Mar;42(3):647-53. [Content Brief]

[2]. Ghosh GC, et al. Oseltamivir carboxylate, the active metabolite of oseltamivir phosphate (Tamiflu), detected in sewage discharge and river water in Japan. Environ Health Perspect. 2010 Jan;118(1):103-7. [Content Brief]

[3]. Ferraris O, et al. Sensitivity of influenza viruses to zanamivir and oseltamivir: a study performed on viruses circulating in France prior to the introduction of neuraminidase inhibitors in clinical practice. Antiviral Res. 2005 Oct;68(1):43-8. [Content Brief]

[4]. Gubareva LV, et al. Comparison of the activities of zanamivir, oseltamivir, and RWJ-270201 against clinical isolates of influenza virus and neuraminidase inhibitor-resistant variants.Antimicrob Agents Chemother. 2001 Dec;45(12):3403-8. [Content Brief]

[5]. Yen HL, et al. Virulence may determine the necessary duration and dosage of oseltamivir treatment for highly pathogenic A/Vietnam/1203/04 influenza virus in mice. J Infect Dis. 2005 Aug 15;192(4):665-72. [Content Brief]

[6]. Hoffmann G, et al. Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system. Antimicrob Agents Chemother. 2009 Nov;53(11):4753-61. [Content Brief]

Animal Administration ^[3]^[4]	Mice^[3] Female 6-week-old BALB/c mice are anesthetized with isofluorane and intranasally inoculated with 50 μL of 10-fold serial dilutions of VN1203/04 virus in PBS. The mouse lethal dose (MLD₅₀) is calculated after a 16-day observation period. Oseltamivir is administered by oral gavage twice daily for 5 or 8 days to groups of 10 mice at dosages of 0.1, 1, and 10 mg/kg/day. Control (infected but untreated) mice received sterile PBS (placebo) on the same schedule. Four hours after the first dose of Oseltamivir, the mice are inoculated intranasally with 5 MLD₅₀ of VN1203/04 virus in 50 μL of PBS. Survival and weight change are observed for 24 days. Virus titers in the mouse organs are determined on days 3, 6, and 9 after inoculation. Three mice from each experimental and placebo group are killed, and the lungs and brains are removed. The organs are homogenized and suspended in 1 mL of PBS. The cellular debris is cleared by centrifugation at 2000 g for 5 min. The limit of virus detection is 0.75 log₁₀ EID₅₀. For calculation of the mean, samples with a virus titer <0.75 log₁₀ EID₅₀/mL are assigned a value of 0. Virus titers in each organ are calculated by use of the method of Reed and Muench and are expressed as mean log₁₀ EID₅₀/mL±SE. Rats^[4] Several studies are performed to characterize the pharmacokinetics of Oseltamivir and OC in the plasma, cerebrospinal fluid (CSF), and brain of Sprague-Dawley rats following single-dose bolus administration of Oseltamivir (intravenous [i.v.] and oral) and OC (i.v.). In the i.v. studies, nonfasted adult rats (two groups of 35 animals for each test substance) received a dose of 30 mg/kg body weight of either Oseltamivir or Oseltamivir carboxylate (OC) in aqueous solution with sodium chloride (0.9%; pH 4.0) via slow injection into the tail vein over 20 to 30 s. In both i.v. studies, pharmacokinetic sampling took place at 5 min and at 0.25, 0.5, 1, 2, 4, and 8 h postdose (four or five rats/time point). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Li W, et al. Identification of GS 4104 as an orally bioavailable prodrug of the influenza virus neuraminidase inhibitor GS 4071. Antimicrob Agents Chemother. 1998 Mar;42(3):647-53. [Content Brief] [2]. Ghosh GC, et al. Oseltamivir carboxylate, the active metabolite of oseltamivir phosphate (Tamiflu), detected in sewage discharge and river water in Japan. Environ Health Perspect. 2010 Jan;118(1):103-7. [Content Brief] [3]. Ferraris O, et al. Sensitivity of influenza viruses to zanamivir and oseltamivir: a study performed on viruses circulating in France prior to the introduction of neuraminidase inhibitors in clinical practice. Antiviral Res. 2005 Oct;68(1):43-8. [Content Brief] [4]. Gubareva LV, et al. Comparison of the activities of zanamivir, oseltamivir, and RWJ-270201 against clinical isolates of influenza virus and neuraminidase inhibitor-resistant variants.Antimicrob Agents Chemother. 2001 Dec;45(12):3403-8. [Content Brief] [5]. Yen HL, et al. Virulence may determine the necessary duration and dosage of oseltamivir treatment for highly pathogenic A/Vietnam/1203/04 influenza virus in mice. J Infect Dis. 2005 Aug 15;192(4):665-72. [Content Brief] [6]. Hoffmann G, et al. Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system. Antimicrob Agents Chemother. 2009 Nov;53(11):4753-61. [Content Brief]

Animal Administration
^[3]^[4]

Mice^[3]
Female 6-week-old BALB/c mice are anesthetized with isofluorane and intranasally inoculated with 50 μL of 10-fold serial dilutions of VN1203/04 virus in PBS. The mouse lethal dose (MLD₅₀) is calculated after a 16-day observation period. Oseltamivir is administered by oral gavage twice daily for 5 or 8 days to groups of 10 mice at dosages of 0.1, 1, and 10 mg/kg/day. Control (infected but untreated) mice received sterile PBS (placebo) on the same schedule. Four hours after the first dose of Oseltamivir, the mice are inoculated intranasally with 5 MLD₅₀ of VN1203/04 virus in 50 μL of PBS. Survival and weight change are observed for 24 days. Virus titers in the mouse organs are determined on days 3, 6, and 9 after inoculation. Three mice from each experimental and placebo group are killed, and the lungs and brains are removed. The organs are homogenized and suspended in 1 mL of PBS. The cellular debris is cleared by centrifugation at 2000 g for 5 min. The limit of virus detection is 0.75 log₁₀ EID₅₀. For calculation of the mean, samples with a virus titer <0.75 log₁₀ EID₅₀/mL are assigned a value of 0. Virus titers in each organ are calculated by use of the method of Reed and Muench and are expressed as mean log₁₀ EID₅₀/mL±SE.
Rats^[4]
Several studies are performed to characterize the pharmacokinetics of Oseltamivir and OC in the plasma, cerebrospinal fluid (CSF), and brain of Sprague-Dawley rats following single-dose bolus administration of Oseltamivir (intravenous [i.v.] and oral) and OC (i.v.). In the i.v. studies, nonfasted adult rats (two groups of 35 animals for each test substance) received a dose of 30 mg/kg body weight of either Oseltamivir or Oseltamivir carboxylate (OC) in aqueous solution with sodium chloride (0.9%; pH 4.0) via slow injection into the tail vein over 20 to 30 s. In both i.v. studies, pharmacokinetic sampling took place at 5 min and at 0.25, 0.5, 1, 2, 4, and 8 h postdose (four or five rats/time point).

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

参考文献

[1]. Li W, et al. Identification of GS 4104 as an orally bioavailable prodrug of the influenza virus neuraminidase inhibitor GS 4071. Antimicrob Agents Chemother. 1998 Mar;42(3):647-53. [Content Brief]

[2]. Ghosh GC, et al. Oseltamivir carboxylate, the active metabolite of oseltamivir phosphate (Tamiflu), detected in sewage discharge and river water in Japan. Environ Health Perspect. 2010 Jan;118(1):103-7. [Content Brief]

[3]. Ferraris O, et al. Sensitivity of influenza viruses to zanamivir and oseltamivir: a study performed on viruses circulating in France prior to the introduction of neuraminidase inhibitors in clinical practice. Antiviral Res. 2005 Oct;68(1):43-8. [Content Brief]

[4]. Gubareva LV, et al. Comparison of the activities of zanamivir, oseltamivir, and RWJ-270201 against clinical isolates of influenza virus and neuraminidase inhibitor-resistant variants.Antimicrob Agents Chemother. 2001 Dec;45(12):3403-8. [Content Brief]

[5]. Yen HL, et al. Virulence may determine the necessary duration and dosage of oseltamivir treatment for highly pathogenic A/Vietnam/1203/04 influenza virus in mice. J Infect Dis. 2005 Aug 15;192(4):665-72. [Content Brief]

[6]. Hoffmann G, et al. Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system. Antimicrob Agents Chemother. 2009 Nov;53(11):4753-61. [Content Brief]

Oseltamivir acid 相关分类

Infection

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

DMSO / H₂O	1 mM	3.5168 mL	17.5840 mL	35.1679 mL	87.9198 mL
	5 mM	0.7034 mL	3.5168 mL	7.0336 mL	17.5840 mL
	10 mM	0.3517 mL	1.7584 mL	3.5168 mL	8.7920 mL
	15 mM	0.2345 mL	1.1723 mL	2.3445 mL	5.8613 mL
	20 mM	0.1758 mL	0.8792 mL	1.7584 mL	4.3960 mL
	25 mM	0.1407 mL	0.7034 mL	1.4067 mL	3.5168 mL
	30 mM	0.1172 mL	0.5861 mL	1.1723 mL	2.9307 mL
	40 mM	0.0879 mL	0.4396 mL	0.8792 mL	2.1980 mL
	50 mM	0.0703 mL	0.3517 mL	0.7034 mL	1.7584 mL
	60 mM	0.0586 mL	0.2931 mL	0.5861 mL	1.4653 mL
	80 mM	0.0440 mL	0.2198 mL	0.4396 mL	1.0990 mL
	100 mM	0.0352 mL	0.1758 mL	0.3517 mL	0.8792 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:

Oseltamivir acid187227-45-8GS 4071 Ro 64-0802 Oseltamivir carboxylate奥斯他伟酸GS4071GS-4071Influenza VirusDrug MetaboliteInhibitorinhibitorinhibit

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Oseltamivir acid (Synonyms: 奥斯他伟酸; GS 4071; Ro 64-0802; Oseltamivir carboxylate)

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Oseltamivir acid (Synonyms: 奥斯他伟酸; GS 4071; Ro 64-0802; Oseltamivir carboxylate)

Customer Review

Other Forms of Oseltamivir acid:

Oseltamivir acid 相关抗体

MCE 顾客使用本产品发表的 71 篇科研文献

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