GS-9256

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GS-9256

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1001094-46-7

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

GS-9256 是一种选择性的HCV NS3蛋白酶抑制剂。GS-9256 具有良好的药代动力学特性和抗病毒活性。

生物活性

GS-9256 is a selectiveHCVNS3protease inhibitor. GS-9256 has good pharmacokinetic properties and antiviral activity^[1].

体外研究
(In Vitro)

GS-9256 (0.002-0.183 μM) has a mean EC₅₀value of 20 nM in GT1b huh-luc cells with a replicon encoding luciferase^[1].
GS-9256 (3 μM) retains wild-type activity against all NS5B and NS5A inhibitor-resistant mutations tested and is metabolically stable in microsomes and hepatocytes including rodents, dogs and humans^[1].

体内研究
(In Vivo)

GS-9256 (1 mg/kg, i.v., 30 min) is highly bioavailable in mice (near 100%) and moderately bioavailable in rats (14%), dogs (21%) and monkeys (14%). The elimination half-life is approximately 2 hours in mice, 0.6 hours in rats, 5 hours in dogs, and 4 hours in monkeys^[1].
The pharmacokinetic parameters of GS-9256(IV, 2 mg/kg mouse and 1 mg/kg rat, dog, monkey; Oral, 50 mg/kg mouse, 5 mg/kg rat and monkey, 4 mg/kg dog)

-	Parameters	CD-1 mouse	Sprague Dawley rat	Beagle dog	Cynomolgus monkey
Intravenous	CL(L/h/kg)	2.0	1.26	0.04	0.33
	Vss (L/kg)	2.3	0.16	0.09	0.27
	t_1/2(h)	2.35	0.61	4.88	3.95
	MRT(h)	1.15	0.13	2.11	0.82
Oral	T_max(h)	3.00	0.67	2.00	2.67
	C_max(nM)	11116	265	4369	604
	t_1/2(h)	1.31	0.53	4.22	4.42
	AUC_0-∞(nM*h)	58959	445	21043	2304
	F(%)	Complete	13.9	21	14

Clinical Trial

分子量

957.46

Formula

C₄₆H₅₆ClF₂N₆O₈PS

CAS 号

1001094-46-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.