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Grazoprevir

Catalog No. T4547   CAS 1350514-68-9
Synonyms: MK-5172

Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Ki of 0.01 nM (gt1a), 0.08 nM (gt2a), 0.90 nM (gt3a), 0.01 nM (gt1b), 0.15 nM (gt2b), respectively.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Grazoprevir Chemical Structure
Grazoprevir, CAS 1350514-68-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 41.00
2 mg In stock $ 59.00
5 mg In stock $ 96.00
10 mg In stock $ 148.00
25 mg In stock $ 283.00
50 mg In stock $ 492.00
100 mg In stock $ 712.00
500 mg In stock $ 1,460.00
1 mL * 10 mM (in DMSO) In stock $ 127.00
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Purity: 100%
Purity: 99.99%
Purity: 99.36%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Ki of 0.01 nM (gt1a), 0.08 nM (gt2a), 0.90 nM (gt3a), 0.01 nM (gt1b), 0.15 nM (gt2b), respectively.
Targets&IC50 GT1a:0.01 nM (Ki), GT1b:0.01 nM (Ki), gt2a:0.08 nM (Ki), gt2b:0.15 nM (Ki), gt3a:0.90 nM (Ki)
In vitro In biochemical assays, MK-5172 is effective against a panel of major genotypes and variants engineered with common resistant mutations, with Ki of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), 0.07 nM (gt1bR155K), 0.14 nM (gt1bD168V), 0.30 nM (gt1bD168Y), 5.3 nM (gt1bA156T), and 12 nM (gt1bA156V), respectively. In the replicon assay, MK-5172 demonstrates subnanomolar to low-nanomolar EC50s against genotypes 1a, 1b, and 2a, with EC50s of 0.5±0.1 nM, 2±1 nM, and 2±1 nM for gt1bcon1, gt1a, and gt2a, respectively. MK-5172 is potent against a panel of HCV replication mutants NS5A (Y93H) (EC50: 0.7 nM), NS5B nucleosides (S282T) (EC50: 0.3 nM), and NS5B (C316Y) (EC50: 0.4 nM)[1]. MK-5172 maintains the excellent potency against the gt 3a enzyme as well as a broad panel of mutant enzymes, has excellent potency in the replicon system [gt1b IC50(50% NHS): 7.4 nM; gt1a IC50(40% NHS): 7 nM], and shows excellent rat liver exposure[2].
In vivo When dosed to dogs, MK-5172 shows low clearance of 5 mL/min/kg and a 3 h half-life after iv dosing and has good plasma exposure (AUC: 0.4 μM/h) after a 1 mg/kg oral dose. Dog liver biopsy studies showed that the liver concentration of MK-5172 after the 1 mg/kg oral dose is 1.4 μM at the 24 h time point. Similar to its behaviour in rats, MK-5172 demonstrates effective partitioning into liver tissue and maintains high liver concentration, relative to potency, 24 h after oral dosing in dogs [2].
Synonyms MK-5172
Molecular Weight 766.9
Formula C38H50N6O9S
CAS No. 1350514-68-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (71.72 mM)

Ethanol: 15 mg/mL

TargetMolReferences and Literature

1. Summa V, et al. MK-5172, a selective inhibitor of hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants. Antimicrob Agents Chemother. 2012 Aug;56(8):4161-7. 2. Harper S, et al. Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor. ACS Med Chem Lett. 2012 Mar 2;3(4):332-6.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Aging Compound Library Inhibitor Library FDA-Approved Drug Library Drug Repurposing Compound Library Clinical Compound Library Approved Drug Library NO PAINS Compound Library Bioactive Compound Library Target-Focused Phenotypic Screening Library Anti-Infection Compound Library

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Keywords

Grazoprevir 1350514-68-9 Microbiology/Virology Proteases/Proteasome HCV Protease SARS-CoV Hepatitis C virus MK5172 HCV Inhibitor inhibit MK 5172 MK-5172 SARS coronavirus inhibitor

 

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