| 产品描述: | DPC-681 is a potent and selective HIV protease inhibitor (IC90s: 4 to 40 nM for wild-type HIV-1). |
| 体外研究: |
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. |
| 体内研究: |
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 |
| 参考文献: |
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. |
| 溶解性: |
10 mM in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.493 ml |
7.464 ml |
14.929 ml |
| 5 mM |
0.299 ml |
1.493 ml |
2.986 ml |
| 10 mM |
0.149 ml |
0.746 ml |
1.493 ml |
| 50 mM |
0.03 ml |
0.149 ml |
0.299 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |