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Paritaprevir dihydrate
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。
Paritaprevir dihydrate图片
CAS NO:1456607-71-8
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
ABT-450 dihydrate
Veruprevir dihydrate
产品介绍
Paritaprevir (ABT-450) dihydrate 是一种有效且具有口服活性和抗病毒活性的非结构蛋白 3/4A (NS3/4A) 蛋白酶抑制剂,对 HCV 1a 和 1b 的EC50分别为 1 和 0.21 nM。Paritaprevir dihydrate 也是一种SARS-CoV3CLpro抑制剂,IC50为1.31 μM。Paritaprevir dihydrate 主要由细胞色素 P450 (CYP) 3A 代谢。利托那韦 (Ritonavir,一种 CYP450 抑制剂) 可提高 Paritaprevir dihydrate 的血浆浓度和半衰期。
生物活性

Paritaprevir (ABT-450) dihydrate is a potent, orally active and antiviralnon-structural protein 3/4A (NS3/4A) proteaseinhibitor with EC50s of 1 and 0.21 nM againstHCV1a and 1b, respectively. Paritaprevir dihydrate is also aSARS-CoV3CLproinhibitor with an IC50of 1.31 μM. Paritaprevir dihydrate is metabolized primarily bycytochrome P450(CYP) 3A. The plasma concentration and half-life of Paritaprevir dihydrate can be enhanced byRitonavir(a CYP450 inhibitor)[1][2][3][4].

IC50& Target

EC50: 1 nM (HCV 1a), 0.21 nM (HCV 1b)[1]
IC50: 1.31 μM (SARS-CoV 3CLpro)[3]

体外研究
(In Vitro)

Paritaprevir hasin vitroantiviral activity against HCV GT1-4 and GT6 (EC50range, 0.09 to 19 nM), with an EC50of 0.09 nM against GT4a[2].

体内研究
(In Vivo)

The combination of Paritaprevir,Ritonavir,Ombitasvir(an NS5A protein inhibitor), andDasabuvir(an NS5B non-nucleoside polymerase inhibitor) with or without RBV has been approved to treat HCV genotype 1 infections[1][4].
The acute toxicity of Paritaprevir is considered to be low. Single oral doses of ≤600 mg/kg in rats and ≤100 mg/kg in dogs produces no mortality and were well tolerated. However, since Paritaprevir is administered without ritonavir as a PK enhancer, the exposures are low, especially in male rats (rat 600 mg/kg, males: Cmax1.82 μg/mL, AUC0-248.89 μg·h/mL; dog 100 mg/kg, mean: Cmax61.3 μg/mL, AUC0-24285 μg·h/mL).

Clinical Trial
分子量

801.91

Formula

C40H47N7O9S

CAS 号

1456607-71-8

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.