Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GS-9256 is a selective inhibitor of the HCV NS3 protease, exhibiting favorable pharmacokinetic properties and antiviral activity [1].
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
25 mg | 約6-8 週間 | ¥ 349,000 |
50 mg | 約6-8 週間 | ¥ 454,500 |
100 mg | 約6-8 週間 | ¥ 574,000 |
説明 | GS-9256 is a selective inhibitor of the HCV NS3 protease, exhibiting favorable pharmacokinetic properties and antiviral activity [1]. |
In vitro | GS-9256 demonstrates potent antiviral activity with a mean EC50 of 20 nM across a concentration range of 0.002-0.183 μM in GT1b huh-luc cells harboring a luciferase-encoding replicon [1]. Furthermore, at 3 μM, GS-9256 maintains efficacy against all tested resistant mutations in NS5B and NS5A inhibitors, showcasing its metabolic stability in microsomes and hepatocytes from rodents, dogs, and humans [1]. |
In vivo | GS-9256 exhibits high bioavailability in mice (approximately 100%) when administered intravenously at 1 mg/kg with a 30-minute exposure, while showing moderate bioavailability in rats (14%), dogs (21%), and monkeys (14%). The compound's elimination half-life spans approximately 2 hours in mice, 0.6 hours in rats, 5 hours in dogs, and 4 hours in monkeys. Regarding the pharmacokinetic parameters at indicated doses for each species (IV: 2 mg/kg in mice, 1 mg/kg in rats, dogs, and monkeys; Oral: 50 mg/kg in mice, 5 mg/kg in rats and monkeys, and 4 mg/kg in dogs), they are as follows: for the CD-1 mouse, Sprague-Dawley rat, Beagle dog, and Cynomolgus monkey, the clearance (CL) is 2.0, 1.26, 0.04, and 0.33 L/h/kg respectively, while the volume of distribution at steady state (Vss) is 2.3, 0.16, 0.09, and 0.27 L/kg respectively [1]. |
分子量 | 957.46 |
分子式 | C46H56ClF2N6O8PS |
CAS No. | 1001094-46-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. 詳細
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
GS-9256 1001094-46-7 Microbiology/Virology Proteases/Proteasome HCV Protease GS 9256 GS9256 KX-1141 KX 1141. Inhibitor inhibitor inhibit