製品番号: HY-13337

BMS-986094

Name: BMS-986094
Brand: MedChemExpress
SKU: HY-13337
Price: 190.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(別名: INX-08189)

カスタマーレビュー

Based on 1 Customer Validation

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.88%
CAS 番号: 1234490-83-5
分子式: C₃₀H₃₉N₆O₉P
分子量:658.64

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

BMS-986094 構造式

CAS 番号: 1234490-83-5

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

HY-10443
Balapiravir

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

EC50: 35 nM (HCV)^[1]

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	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: 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]
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	6 μM Compound: 3	Cytotoxicity against human HuH7 cells Cytotoxicity against human HuH7 cells	[PMID: 23453067]
Huh-7	CC₅₀	7 μM Compound: 4g	Cytotoxicity against human HuH7 cells Cytotoxicity against human HuH7 cells	[PMID: 20637609]
Huh-7	CC₅₀	7 μM Compound: 7b	Cytotoxicity against human HuH7 cells Cytotoxicity against human HuH7 cells	[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	0.01 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	0.02 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]
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: 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]
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]

体外実験

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].

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

体内実験

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].

MedChemExpress (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.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1234490-83-5
性状 Solid
分子量 658.64
分子式 C₃₀H₃₉N₆O₉P
Color White to off-white
SMILES

C[C@]([C@](O[C@@H]1CO[P](OC2=CC=CC3=C2C=CC=C3)(N[C@@H](C)C(OCC(C)(C)C)=O)=O)([H])N4C5=NC(N)=NC(OC)=C5N=C4)([C@@H]1O)O
別名

INX-08189
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 250 mg/mL (379.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (3.16 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.16 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
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HNMR (2659 KB)
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MS (2659 KB)
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OR (2659 KB)
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取扱説明書 (2659 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	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

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BMS-986094

生物活性