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编 号:F076221
分子式:C40H43N7O7S
分子量:765.88
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10mM*1mL in DMSO
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2mg
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5mg
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10mg
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50mg
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100mg
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生物活性:
Paritaprevir (ABT-450) is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.31 μM. Paritaprevir is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir can be enhanced by Ritonavir (a CYP450 inhibitor).

体内研究:
The combination of Paritaprevir, Ritonavir, Ombitasvir (an NS5A protein inhibitor), and Dasabuvir (an NS5B non-nucleoside polymerase inhibitor) with or without RBV has been approved to treat HCV genotype 1 infections.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: Cmax 1.82 μg/mL, AUC0-24 8.89 μg·h/mL; dog 100 mg/kg, mean: Cmax 61.3 μg/mL, AUC0-24 285 μg·h/mL).

体外研究:
Paritaprevir has in vitro antiviral activity against HCV GT1-4 and GT6 (EC50 range, 0.09 to 19 nM), with an EC50 of 0.09 nM against GT4a.
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