化合物 T15163 T15163

Product Introduction
Bioactivity


英文名: DPC-681

描述: DPC-681 is a potent and selective HIV protease inhibitor (IC90s: 4 to 40 nM for wild-type HIV-1).

体外活性: DPC 681 displays no loss in potency toward recombinant mutant HIVs with the D30N mutation and a fivefold or smaller loss in potency toward mutant variants with three to five amino acid substitutions. When all of the HIV-1 strains tested are considered, the average concentrations required for 90% inhibition of replication were 7.3 ± 3.4 for DPC 681.

体内活性: The total body clearance (CL) of DPC 681 in dogs was high (1.8 liters/h/kg) equaling hepatic blood flow for this species (1.8 liters/h/kg). The Cmax increased ninefold between the 10- and 30-mg/kg DPC 681 dose groups. Bioavailability also increased between the 10- and 30-mg/kg dose groups (18.3 and 78.1%, respectively), after oral dosing. These data show that hepatic extraction (first-pass effect) can be saturated in the dog.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: DPH 153893 | DPC-681 | DPC 681 | DPC681 | DPH153893

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途