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MK-5172

HY-15298

(Grazoprevir; MK 5172; MK5172)

MK-5172

MK-5172 Chemical Structure

MK-5172 is a novel P2-P4 quinoxaline macrocyclic HCV NS3/4a protease inhibitor currently in clinical development.

Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO $118 In-stock
5 mg $90 In-stock
10 mg $140 In-stock
50 mg $450 In-stock
100 mg $650 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €116 In-stock
5 mg €88 In-stock
10 mg €137 In-stock
50 mg €441 In-stock
100 mg €637 In-stock
200 mg Get quote
500 mg Get quote

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Product name: MK-5172
Cat. No.: HY-15298

MK-5172 Data Sheet

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    Purity: 99.24%

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    DataSheet

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    COA

Related Compound Libraries

Biological Activity of MK-5172

MK-5172 is a novel P2-P4 quinoxaline macrocyclic HCV NS3/4a protease inhibitor currently in clinical development.
IC50 Value: 7.4 nM and 7 nM for genotype 1b and 1a respectively, in replicon system [1]
Target: HCV NS3/4a protease
in vitro: In biochemical assays, MK-5172 was effective against a panel of major genotypes and variants engineered with common resistant mutations observed in clinical studies with other NS3/4a protease inhibitors. In the replicon assay, MK-5172 demonstrated subnanomolar to low-nanomolar EC50s against genotypes 1a, 1b, and 2a [2].
in vivo: In rats, MK-5172 showed a plasma clearance of 28 ml/min/kg and plasma half-life of 1.4 hr. When dosed p.o. at 5 mg/kg, the plasma exposure of MK-5172 was good with an AUC of 0.7 uM.hr. The liver exposure of the compound was quite good (23 uM at 4 hr), and MK-5172 remained in liver 24 hr after a single p.o. 5 mg/kg dose. At 24 hr, the liver concentration of MK-5172 was 0.2 uM, which was over 25-fold higher than the IC50 in the replicon assay with 50% NHS. When dosed to dogs, MK-5172 showed low clearance of 5 ml/min/kg and a 3 hr half-life after i.v. 2 mg/kg dosing and had good plasma exposure (AUC=0.4 uM.hr) after a p.o. 1 mg/kg dose [1].
Clinical trial: Evaluation of Hepatic Pharmacokinetics for MK-5172 in Participants With Chronic Hepatitis C . Phase1
 

Chemical Information

M.Wt 766.9 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C38H50N6O9S
CAS No 1350514-68-9
Solvent & Solubility

10 mM in DMSO

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 1.3040 mL 6.5198 mL 13.0395 mL
5 mM 0.2608 mL 1.3040 mL 2.6079 mL
10 mM 0.1304 mL 0.6520 mL 1.3040 mL

Clinical Information of MK-5172

Product Name Sponsor Only Condition Start Date End Date Phase Last Change Date
MK-5172 Merck & Co Inc Hepatitis C virus infection 31-JAN-13 30-APR-14 Phase 2 12-SEP-13
Merck & Co Inc Hepatitis C virus infection 28-FEB-13 31-AUG-14 Phase 2 19-NOV-13
Merck & Co Inc Hepatitis C virus infection 31-DEC-12 31-JAN-14 Phase 2 04-NOV-13
Merck & Co Inc Hepatitis C virus infection 31-OCT-13 30-SEP-14 Phase 2 23-OCT-13

References on MK-5172

Other Forms

Inhibitor Kit

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