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DPC-681(DPH-153893)
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。
DPC-681(DPH-153893)图片
CAS NO:284661-68-3
规格:98%
分子量:669.85
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
DPC-681是一种有效的选择性HIVprotease抑制剂,抑制野生型HIV-1IC90值为4-40nM。
CAS:284661-68-3
分子式:C35H48FN5O5S
分子量:669.85
纯度:98%
存储:Store at -20°C

Background:

DPC-681 is a potent and selective inhibitor of HIV protease with IC90s for wild-type HIV-1 of 4 to 40 nM.IC50 value: 4 - 40 nM [1]Target: HIV proteasein vitro: DPC 681 is extremely potent inhibitor of wild-type HIV-1. 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. DPC 681 shows 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. [1]in vivo: The total body clearance (CL) of DPC 681 in dogs was high (1.8 liter/h/kg) equaling hepatic blood flow for this species (1.8 liter/h/kg). After an oral dosing, 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). These data suggest that hepatic extraction (first-pass effect) can be saturated in the dog. [1]




[1]. Kaltenbach RF 3rd, et al. DPC 681 and DPC 684: potent, selective inhibitors of human immunodeficiency virus protease active against clinically relevant mutant variants. Antimicrob Agents Chemother. 2001 Nov;45(11):3021-8.