1. Anti-infection
    Metabolic Enzyme/Protease
  2. HCV
    HCV Protease
    SARS-CoV
  3. Grazoprevir hydrate

Grazoprevir hydrate (Synonyms: MK-5172 hydrate)

Cat. No.: HY-15298B Purity: 99.10%
Handling Instructions

Grazoprevir hydrate (MK-5172 hydrate) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively. Grazoprevir hydrate inhibits SARS-CoV-2 3CLpro activity.

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

Grazoprevir hydrate Chemical Structure

Grazoprevir hydrate Chemical Structure

CAS No. : 1350462-55-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 145 In-stock
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 168 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 780 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of Grazoprevir hydrate:

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Description

Grazoprevir hydrate (MK-5172 hydrate) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively[1][2]. Grazoprevir hydrate inhibits SARS-CoV-2 3CLpro activity[3].

IC50 & Target

Ki: 0.01±<0.01 nM (gt1b), 0.01±0.01 nM (gt1a), 0.08±0.02 nM (gt2a), 0.15±0.06 nM (gt2b), 0.90±0.2 nM (gt3a)[1]

In Vitro

In biochemical assays, Grazoprevir (MK-5172) is effective against a panel of major genotypes and variants engineered with common resistant mutations, with Ki of 0.01±<0.01 nM (gt1b), 0.01±0.01 nM (gt1a), 0.08±0.02 nM (gt2a), 0.15±0.06 nM (gt2b), 0.90±0.2 nM (gt3a), 0.07±0.01 nM (gt1bR155K), 0.14±0.03 nM (gt1bD168V), 0.30±0.04 nM (gt1bD168Y), 5.3±0.9 nM (gt1bA156T), and 12±2 nM (gt1bA156V), respectively. In the replicon assay, Grazoprevir 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. Grazoprevir is potent against a panel of HCV replication mutants NS5A (Y93H) (EC50=0.7±0.3 nM), NS5B nucleosides (S282T) (EC50=0.3±0.1 nM), and NS5B (C316Y) (EC50=0.4±0.2)[1]. Grazoprevir (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].

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

In Vivo

Grazoprevir (MK-5172) demonstrates efficacy in vivo against chronic-HCV-infected chimpanzees[1]. When dosed to dogs, Grazoprevir (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 Grazoprevir after the 1 mg/kg oral dose is 1.4 μM at the 24 h time point. Similar to its behavior in rats, Grazoprevir demonstrates effective partitioning into liver tissue and maintains high liver concentration, relative to potency, 24 h after oral dosing in dogs[2].

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

Clinical Trial
Molecular Weight

784.92

Formula

C₃₈H₅₂N₆O₁₀S

CAS No.
SMILES

COC1=CC2=C(N=C(CCCCC[[email protected]@H]3C[[email protected]]3OC4=O)C(O[[email protected]]5CN(C([[email protected]](C(C)(C)C)N4)=O)[[email protected]](C(N[[email protected]@]([[email protected]@H]6C=C)(C6)C(NS(C7CC7)(=O)=O)=O)=O)C5)=N2)C=C1.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 : 50 mg/mL (63.70 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2740 mL 6.3701 mL 12.7402 mL
5 mM 0.2548 mL 1.2740 mL 2.5480 mL
10 mM 0.1274 mL 0.6370 mL 1.2740 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.19 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (3.19 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

GrazoprevirMK-5172MK5172MK 5172HCVHCV ProteaseSARS-CoVHepatitis C virusSARS coronavirusInhibitorinhibitorinhibit

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Product Name:
Grazoprevir hydrate
Cat. No.:
HY-15298B
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