MK-5172 sodium salt

MK-5172 sodium salt (MK-5172 sodium salt) 是丙型肝炎病毒 NS3/4a 蛋白酶的选择性抑制剂，对基因型和耐药变异具有广泛的活性，Kis 为 0.01 nM (gt1b)、0.01 nM (gt1a)、0.08 nM (gt2a)、0.15 nM (gt2b)、0.90 nM (gt3a)。

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库存: 现货

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5mg

￥850.00

680.00

- +
10mg

￥1225.00

980.00

- +
50mg

￥3700.00

2960.00

- +
100mg

￥5400.00

4320.00

- +

已选 0 种 0 瓶

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货号: ajci7168
CAS: 1425038-27-2
别名: MK5172 sodium salt;MK 5172 sodium salt
分子式: C38H50N6NaO9S+
分子量: 789.89
纯度: >98%
溶解度: Soluble in DMSO
储存: Store at -20°C
库存: 现货

Background

IC50 Value: 7.4nM and 7nM for genotype1b and 1a respectively, in replicon system [1] MK-5172 is a novel P2-P4 quinoxaline macrocyclic HCV NS3/4a protease inhibitor currently in clinical development. 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