1. Anti-infection
  2. HCV
  3. BMS-986094

BMS-986094 (Synonyms: INX-08189)

Cat. No.: HY-13337 Purity: 99.90%
Handling Instructions

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 prodrug of 6-O-methyl-2’-C-methyl guanosine. BMS-986094 can be used for the research of chronic HCV infection.

For research use only. We do not sell to patients.

BMS-986094 Chemical Structure

BMS-986094 Chemical Structure

CAS No. : 1234490-83-5

Size Price Stock Quantity
5 mg USD 850 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1450 In-stock
Estimated Time of Arrival: December 31
25 mg USD 2800 In-stock
Estimated Time of Arrival: December 31
50 mg USD 4500 In-stock
Estimated Time of Arrival: December 31
100 mg USD 7200 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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 prodrug 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]

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.

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
Molecular Weight

658.64

Formula

C30H39N6O9P

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
References
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BMS-986094
Cat. No.:
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