MK-5172 sodium salt
| CAS号 | 1425038-27-2 | 货号 | BCP13442 |
| 中文名 | MK-5172 sodium salt | ||
| 英文名 | MK-5172 sodium salt | ||
| 中文别名 | |||
| 英文别名 | MK 5172 sodium salt;MK5172 sodium salt; | ||
| 分子式 | C38H50N6NaO9S+ | 分子量 | 789.89 |
| 生物活性 | 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 . | ||
| 信号通路 | Protease/Metabolic Enzyme Microbiology/Virology | ||
| 靶 点 | HCV Protease HCV | ||
结构式
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