BMS-986094 (Synonyms: INX-08189)

目录号: HY-13337 纯度: 99.88%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

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。

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BMS-986094 Chemical Structure

CAS No. : 1234490-83-5

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥2090	In-stock
1 mg	￥863	In-stock
5 mg	￥1900	In-stock
10 mg	￥2400	In-stock
25 mg	￥4900	In-stock
50 mg	现货	询价
100 mg		询价
200 mg		询价

or 大包装询价

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生物活性
纯度 & 产品资料
参考文献

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^[1]^[2].

IC₅₀ & Target

EC50: 35 nM (HCV)^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	CC₅₀	7.8 μM Compound: BMS-986094; INX-08189	Cytotoxicity against human A549 cells treated for 8 days measured post-last dose by Celltiter-glo luminescent assay Cytotoxicity against human A549 cells treated for 8 days measured post-last dose by Celltiter-glo luminescent assay	[PMID: 30951311]
CCRF-CEM	CC₅₀	8 μM Compound: 3; BMS-986094; INX-189	Cytotoxicity against human CEM cells after 6 days by trypan blue exclusion assay Cytotoxicity against human CEM cells after 6 days by trypan blue exclusion assay	[PMID: 26819659]
CCRF-CEM	CC₅₀	8.7 μM Compound: 1, BMS-986094, INX-189	Cytotoxicity against human CEM cells assessed as reduction in cell viability incubated for 5 days by Cell-titer 96 aqueous one solution cell proliferation assay Cytotoxicity against human CEM cells assessed as reduction in cell viability incubated for 5 days by Cell-titer 96 aqueous one solution cell proliferation assay	[PMID: 25849312]
HeLa	CC₅₀	13.4 μM Compound: BMS-986094; INX-08189	Cytotoxicity against human HeLa cells treated for 8 days measured post-last dose by Celltiter-glo luminescent assay Cytotoxicity against human HeLa cells treated for 8 days measured post-last dose by Celltiter-glo luminescent assay	[PMID: 30951311]
HepG2	CC₅₀	< 1 μM Compound: 1, BMS-986094, INX-189	Mitochondrial toxicity in human HepG2 cells assessed as effect on mitochondrial cytochrome c oxidase subunit 2 DNA level incubated for 14 days by real-time PCR method Mitochondrial toxicity in human HepG2 cells assessed as effect on mitochondrial cytochrome c oxidase subunit 2 DNA level incubated for 14 days by real-time PCR method	[PMID: 25849312]
HepG2	CC₅₀	< 1 μM Compound: 1, BMS-986094, INX-189	Mitochondrial toxicity in human HepG2 cells assessed as effect on nuclear beta-actin DNA level incubated for 14 days by real-time PCR method Mitochondrial toxicity in human HepG2 cells assessed as effect on nuclear beta-actin DNA level incubated for 14 days by real-time PCR method	[PMID: 25849312]
HepG2	CC₅₀	1.5 μM Compound: BMS-986094; INX-08189	Cytotoxicity against human HepG2 cells treated for 8 days measured post-last dose by Celltiter-glo luminescent assay Cytotoxicity against human HepG2 cells treated for 8 days measured post-last dose by Celltiter-glo luminescent assay	[PMID: 30951311]
Huh-7	EC₅₀	0.01 μM Compound: 7b	Antiviral activity against Hepatitis C virus subtype 1b replicon in human HuH7 cells after 48 hrs by subgenomic replicon assay Antiviral activity against Hepatitis C virus subtype 1b replicon in human HuH7 cells after 48 hrs by subgenomic replicon assay	[PMID: 21856153]
Huh-7	EC₅₀	0.01 μM Compound: 4g	Antiviral activity against HCV genotype 1b in Huh7 cells assessed as inhibition of viral replication by cell-based replicon assay Antiviral activity against HCV genotype 1b in Huh7 cells assessed as inhibition of viral replication by cell-based replicon assay	[PMID: 20637609]
Huh-7	EC₅₀	0.02 μM Compound: 1, BMS-986094, INX-189	Antiviral activity against HCV infected in human HuH7 cells assessed as reduction in replicon RNA levels incubated for 5 days by RT-PCR assay Antiviral activity against HCV infected in human HuH7 cells assessed as reduction in replicon RNA levels incubated for 5 days by RT-PCR assay	[PMID: 25849312]
Huh-7	CC₅₀	0.35 μM Compound: BMS-986094; INX-08189	Cytotoxicity against human HuH7 cells treated for 8 days measured post-last dose by Celltiter-glo luminescent assay Cytotoxicity against human HuH7 cells treated for 8 days measured post-last dose by Celltiter-glo luminescent assay	[PMID: 30951311]
Huh-7	CC₅₀	0.8 μM Compound: 3; BMS-986094; INX-189	Cytotoxicity against human HuH7 cells infected with HCV assessed as reduction in cellular rRNA level after 96 hrs by qRT-PCR analysis Cytotoxicity against human HuH7 cells infected with HCV assessed as reduction in cellular rRNA level after 96 hrs by qRT-PCR analysis	[PMID: 26819659]
Huh-7	CC₅₀	0.8 μM Compound: 1, BMS-986094, INX-189	Cytotoxicity against human HuH7 cells assessed as reduction in rRNA levels incubated for 5 days by RT-PCR assay Cytotoxicity against human HuH7 cells assessed as reduction in rRNA levels incubated for 5 days by RT-PCR assay	[PMID: 25849312]
MT4	CC₅₀	0.96 μM Compound: BMS-986094; INX-08189	Cytotoxicity against human MT4 cells treated for 8 days measured post-last dose by Celltiter-glo luminescent assay Cytotoxicity against human MT4 cells treated for 8 days measured post-last dose by Celltiter-glo luminescent assay	[PMID: 30951311]
PBMC	CC₅₀	4.5 μM Compound: 3; BMS-986094; INX-189	Cytotoxicity against human PBMC after 6 days by trypan blue exclusion assay Cytotoxicity against human PBMC after 6 days by trypan blue exclusion assay	[PMID: 26819659]
PBMC	CC₅₀	4.7 μM Compound: 1, BMS-986094, INX-189	Cytotoxicity against human PBMC assessed as reduction in cell viability incubated for 5 days by Cell-titer 96 aqueous one solution cell proliferation assay Cytotoxicity against human PBMC assessed as reduction in cell viability incubated for 5 days by Cell-titer 96 aqueous one solution cell proliferation assay	[PMID: 25849312]
U-937	CC₅₀	0.17 μM Compound: BMS-986094; INX-08189	Cytotoxicity against human U937 cells treated for 8 days measured post-last dose by Celltiter-glo luminescent assay Cytotoxicity against human U937 cells treated for 8 days measured post-last dose by Celltiter-glo luminescent assay	[PMID: 30951311]
Vero	CC₅₀	14 μM Compound: 3; BMS-986094; INX-189	Cytotoxicity against African green monkey Vero cells after 3 days by hemocytometry Cytotoxicity against African green monkey Vero cells after 3 days by hemocytometry	[PMID: 26819659]
Vero	CC₅₀	14 μM Compound: 1, BMS-986094, INX-189	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 5 days by Cell-titer 96 aqueous one solution cell proliferation assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 5 days by Cell-titer 96 aqueous one solution cell proliferation assay	[PMID: 25849312]

体外研究
(In Vitro)

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^[1].
BMS-986094 (5-80 nM; 14 days) decreases luciferase activity in a concentration-dependent manner in genotype 1b replicon cells^[1].
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^[1].
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^[3].

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

体内研究
(In Vivo)

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^[1].
BMS-986094 (25 mg/kg; p.o.) is efficiently extracts from the portal circulation by the liver following oral administration in cynomolgus monkeys^[1].
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^[3].

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

Animal Model:	Male Sprague-Dawley rats^[1]
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.

Clinical Trial

分子量

658.64

Formula

C₃₀H₃₉N₆O₉P

CAS 号

1234490-83-5

性状

固体

颜色

White to off-white

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 : 250 mg/mL (379.57 mM; 超声助溶; 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	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

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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.16 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（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。
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。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.16 mM); 澄清溶液

此方案可获得 ≥ 2.08 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 20.8 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: 99.88%

选择批次：

Data Sheet (628 KB) SDS (252 KB)

COA (294 KB) LCMS (95 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Vernachio JH, et, al. INX-08189, a phosphoramidate prodrug of 6-O-methyl-2'-C-methyl guanosine, is a potent inhibitor of hepatitis C virus replication with excellent pharmacokinetic and pharmacodynamic properties. Antimicrob Agents Chemother. 2011 May; 55(5): 1843-51. [Content Brief]

[2]. McGuigan C, et, al. Design, synthesis and evaluation of a novel double pro-drug: INX-08189. A new clinical candidate for hepatitis C virus. Bioorg Med Chem Lett. 2010 Aug 15; 20(16): 4850-4. [Content Brief]

[3]. Li W, et, al. In Vitro Metabolite Formation in Human Hepatocytes and Cardiomyocytes and Metabolism and Tissue Distribution in Monkeys of the 2'-C-Methylguanosine Prodrug BMS-986094. Int J Toxicol. 2017 Jan 1; 1091581816683642. [Content Brief]

BMS-986094 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	1 mM	1.5183 mL	7.5914 mL	15.1828 mL	37.9570 mL
	5 mM	0.3037 mL	1.5183 mL	3.0366 mL	7.5914 mL
	10 mM	0.1518 mL	0.7591 mL	1.5183 mL	3.7957 mL
	15 mM	0.1012 mL	0.5061 mL	1.0122 mL	2.5305 mL
	20 mM	0.0759 mL	0.3796 mL	0.7591 mL	1.8979 mL
	25 mM	0.0607 mL	0.3037 mL	0.6073 mL	1.5183 mL
	30 mM	0.0506 mL	0.2530 mL	0.5061 mL	1.2652 mL
	40 mM	0.0380 mL	0.1898 mL	0.3796 mL	0.9489 mL
	50 mM	0.0304 mL	0.1518 mL	0.3037 mL	0.7591 mL
	60 mM	0.0253 mL	0.1265 mL	0.2530 mL	0.6326 mL
	80 mM	0.0190 mL	0.0949 mL	0.1898 mL	0.4745 mL
	100 mM	0.0152 mL	0.0759 mL	0.1518 mL	0.3796 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:

BMS-9860941234490-83-5INX-08189BMS986094BMS 986094INX08189INX 08189HCVHepatitis C virushepatitisCvirusreplicationphosphoramidateprodruginfectionInhibitorinhibitorinhibit

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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）

BMS-986094 (Synonyms: INX-08189)

Customer Review