1. Anti-infection Metabolic Enzyme/Protease
  2. HCV Protease
  3. GS-9256

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。

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GS-9256 Chemical Structure

GS-9256 Chemical Structure

CAS No. : 1001094-46-7

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GS-9256 is a selective HCV NS3 protease 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 EC50 value 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
t1/2(h) 2.35 0.61 4.88 3.95
MRT(h) 1.15 0.13 2.11 0.82
Oral Tmax(h) 3.00 0.67 2.00 2.67
Cmax(nM) 11116 265 4369 604
t1/2(h) 1.31 0.53 4.22 4.42
AUC0-∞(nM*h) 58959 445 21043 2304
F(%) Complete 13.9 21 14

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

957.46

Formula

C46H56ClF2N6O8PS

CAS 号
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.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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GS-9256
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HY-16593
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