MK-5172|MK5172,cas 1206524-85-7|DC Chemicals

MK-5172|MK5172,cas 1206524-85-7|DC Chemicals

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

Product Name: Grazoprevir(MK-5172)|Cat No. DC9201|cas: 1206524-85-7|Other names: MK 5172; MK5172| Molecule formular: C38H50N6O9SMolecule Weight: 766.9

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.
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. For the detailed information of MK-5172, the solubility of MK-5172 in water, the solubility of MK-5172 in DMSO, the solubility of MK-5172 in PBS buffer, the animal experiment (test) of  MK-5172, the cell expriment (test) of MK-5172, the in vivo, in vitro and clinical trial test of MK-5172, the EC50, IC50,and affinity,of MK-5172, Please contact DC Chemicals.

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