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Products are for research use only. Not for human use. We do not sell to patients.
(Grazoprevir; MK 5172; MK5172)
MK-5172 Chemical Structure
|Product name: MK-5172|
|Cat. No.: HY-15298|
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 
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 .
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 .
Clinical trial: Evaluation of Hepatic Pharmacokinetics for MK-5172 in Participants With Chronic Hepatitis C . Phase1
|M.Wt||766.9||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|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|
|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|
. Summa V, Ludmerer SW, McCauley JA, 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.
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