BMS-986094 INX-08189|cas:1234490-83-5|西域试剂

BMS-986094 INX-08189,99.90%

产品编号：Bellancom-13337| CAS NO：1234490-83-5| 分子式：C₃₀H₃₉N₆O₉P| 分子量：658.64

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货号	价格	库存与货期
Bellancom-13337	￥1900.00	杭州北京（现货）
Bellancom-13337	￥3300.00	杭州北京（现货）
Bellancom-13337	￥6600.00	杭州北京（现货）
Bellancom-13337	￥11500.00	杭州北京（现货）

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BMS-986094 INX-08189

产品介绍

BMS-986094 (INX-08189) 是丙型肝炎病毒 (HCV) 有效抑制剂，在 Huh-7 细胞中，抑制 HCV 复制的 EC₅₀ 值为 35 nM (24 h)。BMS-986094 是 6-O-methyl-2’-C-methyl guanosine 的氨基磷酸酯前体，可用于慢性 HCV 感染的研究。

生物活性

BMS-986094 (INX-08189) is a potent inhibitor of hepatitis C virus (HCV) replication, with an EC₅₀ of 35 nM at 24 h in Huh-7 cells. BMS-986094 is a phosphoramidate proagent of 6-O-methyl-2’-C-methyl guanosine. BMS-986094 can be used for the research of chronic HCV infection.

体外研究

BMS-986094 (INX-08189) is a highly potent inhibitor of HCV replication, with the EC₅₀s of 10 nM against genotype 1b, 12 nM against genotype 1a, and 0.9 nM against genotype 2a after 72 h of exposure. And the concentration resulting in 50% cellular cytotoxicity (CC₅₀) in cultured Huh-7 cells is 7.01 μM.
BMS-986094 (5-80 nM; 14 days) decreases luciferase activity in a concentration-dependent manner in genotype 1b replicon cells.
BMS-986094 (20 μM; 3 days ) decreases relative mitochondrial copy number of 11% in CEM cells. BMS-986094 (1 μM; 14 days ) has no effect on mitochondrial copy number in CEM cells. BMS-986094 does not alter the relative mitochondrial copy number in HepG2 cells.
MS-986094 (10 µM; 24 hours) does not increase apparently in the concentration of BMS-986094 or its metabolites in human hepatocytes (HHs) and human cardiomyocytes (HCMs) except that intracellular concentrations of INX-09114 increases and plateaues after a 7-hour incubation in HCM.

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

体内研究

BMS-986094 (3-300 mg/kg; p.o.) converts to 2′-C-Me-GTP after oral administration, and 2’-C-MeG in the plasma is proportional to the production of 2’-C-MeGTP in the liver.
BMS-986094 (25 mg/kg; p.o.) is efficiently extracts from the portal circulation by the liver following oral administration in cynomolgus monkeys.
BMS-986094 (15 or 30 mg/kg/d; p.o. for 3 weeks) administers cynomolgus monkeys, the nucleoside metabolite M2 was the major plasma analyte, and INX-09114 was the highest drug-related species in the heart and kidney.

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

Animal Model:	Male Sprague-Dawley rats
Dosage:	3, 5, 10, 25 mg/kg
Administration:	A single p.o. administration
Result:	At doses of ≥5 mg/kg, the concentrations of 2′-C-MeGTP in the liver exceeded the EC₉₀ soon after dosing and remained at or above this level for 72 h.

体内研究

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

Animal Model:	Male Sprague-Dawley rats
Dosage:	3, 5, 10, 25 mg/kg
Administration:	A single p.o. administration
Result:	At doses of ≥5 mg/kg, the concentrations of 2′-C-MeGTP in the liver exceeded the EC₉₀ soon after dosing and remained at or above this level for 72 h.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (379.57 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5183 mL	7.5914 mL	15.1828 mL
5 mM	0.3037 mL	1.5183 mL	3.0366 mL
10 mM	0.1518 mL	0.7591 mL	1.5183 mL

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。

In Vivo:

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

1.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.16 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.16 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.16 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.16 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。