Melarsoprol (Synonyms: 美拉胂醇)

目录号: HY-119594 纯度: 98.0%: Data Sheet SDS COA 产品使用指南
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Melarsoprol 是一种三氨基苯胂类三价有机砷，可用于抑制非洲锥虫病。Melarsoprol 通过诱导细胞凋亡 (apoptosis) 来抑制淋巴细胞白血病细胞的生长。Melarsoprol 能够穿过血脑屏障。

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Melarsoprol Chemical Structure

CAS No. : 494-79-1

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5 mg	￥3360	In-stock
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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

生物活性
纯度 & 产品资料
参考文献

生物活性

Melarsoprol, a melaminophenylarsine-type trivalent organic arsenical, is an important agent for African trypanosomiasis. Melarsoprol inhibits the growth of lymphoid leukemic cell by inducing apoptosis. Melarsoprol crosses the blood-brain barrier^[1]^[2]^[3].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
J774	IC₅₀	4.3 μM Compound: S4	Cytotoxicity against J774.1 cell line after 48 hrs Cytotoxicity against J774.1 cell line after 48 hrs	[PMID: 16516467]
L6	IC₅₀	0.005 μg/mL Compound: Melarsoprol	Antitrypanosomal activity against trypomastigotes of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by alamar blue assay Antitrypanosomal activity against trypomastigotes of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by alamar blue assay	[PMID: 22352841]
L6	EC₅₀	0.0075 μM Compound: melarsoprol	Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in rat L6 cells after 72 hrs by alamar blue assay Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in rat L6 cells after 72 hrs by alamar blue assay	[PMID: 22390399]
L6	IC₅₀	0.008 μM Compound: Melarsoprol	Antimicrobial activity against trypomastigote stage of Trypanosoma brucei rhodesiense STIB900 infected in rat L6 cells after 96 hrs by Alamar Blue assay Antimicrobial activity against trypomastigote stage of Trypanosoma brucei rhodesiense STIB900 infected in rat L6 cells after 96 hrs by Alamar Blue assay	[PMID: 24865793]
L6	IC₅₀	0.01 μM Compound: Melarsoprol	Antitrypanosomal activity against blood stream form of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by alamar blue assay Antitrypanosomal activity against blood stream form of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by alamar blue assay	[PMID: 22023653]
L6	IC₅₀	0.013 μM Compound: Melarsoprol	Antiparasitic activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by Alamar blue assay Antiparasitic activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by Alamar blue assay	[PMID: 21937228]
L6	IC₅₀	1.3 μg/mL Compound: Melarsoprol	Cytotoxicity against in rat L6 cells assessed as reduction in cell viability after 70 hrs by alamar blue assay Cytotoxicity against in rat L6 cells assessed as reduction in cell viability after 70 hrs by alamar blue assay	[PMID: 21353728]
L6	IC₅₀	18.3 μM Compound: Melarsoprol	Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay	[PMID: 26237241]
L6	IC₅₀	18.3 μM Compound: Melarsoprol	Cytotoxicity against rat L6 cells assessed as growth inhibition after 72 hrs by inverted microscopy Cytotoxicity against rat L6 cells assessed as growth inhibition after 72 hrs by inverted microscopy	[PMID: 23153330]
L6	IC₅₀	19000 nM Compound: Melarsoprol	Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by MTT assay Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by MTT assay	[PMID: 24398295]
L6	IC₅₀	24.2 μM Compound: Melarsoprol	Cytotoxicity against rat L6 cells assessed as reduction in cell viability measured after 72 hrs by Alamar blue based inverted microscopy analysis Cytotoxicity against rat L6 cells assessed as reduction in cell viability measured after 72 hrs by Alamar blue based inverted microscopy analysis	[PMID: 31784198]
L6	CC₅₀	28.9 μM Compound: MEL	Cytotoxicity against rat L6 cels assessed as reduction in cell viability after 72 hrs by Alamar Blue dye-based fluorometric analysis Cytotoxicity against rat L6 cels assessed as reduction in cell viability after 72 hrs by Alamar Blue dye-based fluorometric analysis	[PMID: 30615444]
L6	IC₅₀	29 μM Compound: Melarsoprol	Cytotoxicity against rat L6 cells assessed as growth inhibition after 72 hrs by alamar blue assay Cytotoxicity against rat L6 cells assessed as growth inhibition after 72 hrs by alamar blue assay	[PMID: 28284860]
L6	IC₅₀	5.1 μM Compound: Melarsoprol	Cytotoxicity against rat L6 cells after 3 days by Alamar blue assay Cytotoxicity against rat L6 cells after 3 days by Alamar blue assay	[PMID: 24956553]
L6	IC₅₀	5.12 μM Compound: MSP	Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay	[PMID: 24268543]
L6	IC₅₀	5.12 μM Compound: MSP, MLSP	Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay	[PMID: 23795673]
L6	IC₅₀	5.12 μM Compound: Melarsoprol	Cytotoxicity against rat L6 cells measured after 70 hrs by alamar blue staining based fluorescence analysis Cytotoxicity against rat L6 cells measured after 70 hrs by alamar blue staining based fluorescence analysis	[PMID: 27102161]
L6	IC₅₀	7.78 mM Compound: MLSP	Cytotoxicity against rat L6 cells after 72 hrs by Alamar blue assay Cytotoxicity against rat L6 cells after 72 hrs by Alamar blue assay	[PMID: 23871911]
L6	IC₅₀	7.78 μM Compound: mel	Cytotoxicity against rat L6 cells after 70 hrs by Alamar blue assay Cytotoxicity against rat L6 cells after 70 hrs by Alamar blue assay	[PMID: 33148495]
L6	IC₅₀	7.78 μM Compound: MEL	Cytotoxicity against rat L6 cells assessed as growth inhibition after 70 hrs by alamar blue assay Cytotoxicity against rat L6 cells assessed as growth inhibition after 70 hrs by alamar blue assay	[PMID: 28031151]
L6	IC₅₀	7.78 μM Compound: MLSP	Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay	[PMID: 19928900]
L6	IC₅₀	7.78 μM Compound: MLSP	Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay	[PMID: 19606902]
L6	IC₅₀	7.78 μM Compound: MAP	Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay	[PMID: 19267462]
L6	IC₅₀	7.78 μM Compound: MEL	Cytotoxicity against rat L6 cells assessed as reduction in cell viability after 72 hrs by Alamar blue assay Cytotoxicity against rat L6 cells assessed as reduction in cell viability after 72 hrs by Alamar blue assay	[PMID: 27344215]
L6	IC₅₀	7.78 μM Compound: Ml	Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay	[PMID: 25746816]
L6	IC₅₀	7.78 μM Compound: Mel	Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay	[PMID: 19395265]
L6	IC₅₀	7.78 μM Compound: Mel	Cytotoxicity against rat L6 cells after 72 hrs by microplate fluorometry Cytotoxicity against rat L6 cells after 72 hrs by microplate fluorometry	[PMID: 23880082]
L6	IC₅₀	7.78 μM Compound: melarsoprol (mel)	Cytotoxicity against rat L6 cells after 72 hrs by microplate alamar blue assay Cytotoxicity against rat L6 cells after 72 hrs by microplate alamar blue assay	[PMID: 18502136]
L6	IC₅₀	7.78 μM Compound: mel	Cytotoxicity against rat L6 cells after 72 hrs by microplate assay Cytotoxicity against rat L6 cells after 72 hrs by microplate assay	[PMID: 17544672]
L6	IC₅₀	7.8 μM Compound: Melarsoprol	Concentration causing cytotoxicity to 50% of L-6 rat skeletal myoblasts Concentration causing cytotoxicity to 50% of L-6 rat skeletal myoblasts	[PMID: 16107157]
L6	IC₅₀	7.9 μM Compound: MLS	Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay	[PMID: 20047276]
MRC5	IC₅₀	7.4 μM Compound: Melarsoprol	Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell growth after 72 hrs Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell growth after 72 hrs	[PMID: 25199582]

体外研究
(In Vitro)

Melarsoprol (1-100 nM; 24-96 h) 可剂量依赖性和时间依赖性地抑制淋巴细胞白血病细胞的存活和生长^[2]。
Melarsoprol (10-100 nM; 24 h) 表现出细胞凋亡的形态学特征^[2]。
Melarsoprol (1-100 nM; 24 h) 可抑制 bcl-2 mRNA 和蛋白的表达^[2]。
WSU-CLL, I83CLL and JVM-2 cells^[2] 10 nM, 100 nM 24 h Showed characteristic apoptotic changes, such as chromatin condensation and fragmentation, membrane blebbing, and formation of apoptotic bodies. WSU-CLL, I83CLL and JVM-2 cells^[2] 10 nM, 100 nM 24 h Observed prominent concentration-dependent downregulation of bcl-2 mRNA. I83CLL and WSU-CLL cells^[2] 1 nM, 10 nM, 100 nM 24 h Decrease of bcl-2 protein expression was observed.

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

Cell Viability Assay^[2]

Cell Line:	An Epstein-Barr virus (EBV)-transformed B-prolymphocytic cell line (JVM-2), an EBV-transformed B-cell chronic lymphocytic leukemia (B-CLL) cell line (I83CLL), and one non-EBV-transformed B-CLL cell line (WSU-CLL)
Concentration:	1 nM, 10 nM, 100 nM
Incubation Time:	24 h, 48 h, 96 h
Result:	Caused a dose- and time-dependent inhibition of survival and growth in all three cell lines.

Apoptosis Analysis^[2]

Cell Line:	WSU-CLL, I83CLL and JVM-2 cells
Concentration:	10 nM, 100 nM
Incubation Time:	24 h
Result:	Showed characteristic apoptotic changes, such as chromatin condensation and fragmentation, membrane blebbing, and formation of apoptotic bodies.

RT-PCR^[2]

Cell Line:	WSU-CLL, I83CLL and JVM-2 cells
Concentration:	10 nM, 100 nM
Incubation Time:	24 h
Result:	Observed prominent concentration-dependent downregulation of bcl-2 mRNA.

Western Blot Analysis^[2]

Cell Line:	WSU-CLL, I83CLL and JVM-2 cells
Concentration:	1 nM, 110 nM, 100 nM
Incubation Time:	24 h
Result:	Decrease of bcl-2 protein expression was observed.

体内研究
(In Vivo)

在小鼠中，以对照制剂形式静脉注射 Melarsoprol 溶液 (0.039 mmol/kg) 后，发现其在骨髓中浓度显著升高 (C_max = 1.64 mmol/g)，但脑内浓度却相当高 (C_max = 0.093 mmol/g)，LD₅₀ 为 0.12 mmol/kg^[3]。

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

Clinical Trial

分子量

398.34

Formula

C₁₂H₁₅AsN₆OS₂

CAS 号

494-79-1

性状

固体

颜色

White to off-white

中文名称

美拉胂醇

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	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 36 mg/mL (90.38 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5104 mL	12.5521 mL	25.1042 mL
5 mM	0.5021 mL	2.5104 mL	5.0208 mL
10 mM	0.2510 mL	1.2552 mL	2.5104 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。-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。

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

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动物数量

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工作液所需浓度 : mg/mL

纯度 & 产品资料

纯度: 98.0%

选择批次：

Data Sheet (613 KB) SDS (564 KB)

COA (284 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Z Gregus, et al. Role of glutathione in the biliary excretion of the arsenical drugs trimelarsan and melarsoprol. Biochem Pharmacol. 2000 Jun 1;59(11):1375-85. [Content Brief]

[2]. König A, et al. Comparative activity of melarsoprol and arsenic trioxide in chronic B-cell leukemia lines. Blood. 1997 Jul 15;90(2):562-70. [Content Brief]

[3]. Ben Zirar S, et al. Comparison of nanosuspensions and hydroxypropyl-beta-cyclodextrin complex of melarsoprol: pharmacokinetics and tissue distribution in mice. Eur J Pharm Biopharm. 2008 Oct;70(2):649-56. [Content Brief]

Melarsoprol 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

DMSO	1 mM	2.5104 mL	12.5521 mL	25.1042 mL	62.7605 mL
	5 mM	0.5021 mL	2.5104 mL	5.0208 mL	12.5521 mL
	10 mM	0.2510 mL	1.2552 mL	2.5104 mL	6.2760 mL
	15 mM	0.1674 mL	0.8368 mL	1.6736 mL	4.1840 mL
	20 mM	0.1255 mL	0.6276 mL	1.2552 mL	3.1380 mL
	25 mM	0.1004 mL	0.5021 mL	1.0042 mL	2.5104 mL
	30 mM	0.0837 mL	0.4184 mL	0.8368 mL	2.0920 mL
	40 mM	0.0628 mL	0.3138 mL	0.6276 mL	1.5690 mL
	50 mM	0.0502 mL	0.2510 mL	0.5021 mL	1.2552 mL
	60 mM	0.0418 mL	0.2092 mL	0.4184 mL	1.0460 mL
	80 mM	0.0314 mL	0.1569 mL	0.3138 mL	0.7845 mL

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:

Melarsoprol494-79-1美拉胂醇ParasiteApoptosisMelaminophenylarsinetrivalent organic arsenicalAfrican trypanosomiasisleukemia cellplasma cellmyelomaGSHInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Melarsoprol (Synonyms: 美拉胂醇)