For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>MK-5172 is a novel P2-P4 quinoxaline macrocyclic HCV NS3/4a protease inhibitor currently in clinical development.<br>IC50 Value: 7.4 nM and 7 nM for genotype 1b and 1a respectively, in replicon system [1]<br>Target: HCV NS3/4a protease<br>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].<br>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].<br>Clinical trial: Evaluation of Hepatic Pharmacokinetics for MK-5172 in Participants With Chronic Hepatitis C . Phase1<br></p>
| Catalog Number | I001638 |
| CAS Number | 1425038-27-2 |
| Molecular Formula | C38H50N6NaO9S+ |
| Purity | ≥95% |
| Target | NS3/4a protease |
| Solubility | 10 mM in DMSO |
| Storage | Store at -20°C |
| IC50 | 7.4 nM and 7 nM for genotype 1b and 1a respectively, in replicon system [1] |
| Reference | <p style=/line-height:25px/> |
