产品描述: | Delavirdine (U 90152) mesylate is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine mesylate selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine mesylate is an inhibitor of HIV-1 replication and can can be used for the study of AIDs |
靶点: |
IC50: 0.26 μM (HIV-1 RT); 440 μM (DNA polymerase α); >550 μM (DNA polymerase δ);HIVProtease; ReverseTranscriptase |
体内研究: |
Delavirdine (U 90152) mesylate (oral gavage; 10 mg/kg, 200 mg/kg, 250 mg/kg; single dose) is absorbed and metabolized rapidly, that it constitutes a minor component in circulation, that its pharmacokinetics are nonlinear, and that its metabolism to desalkyl delavirdine is capacity limited or inhibitable in CD-1 mice (PK study) |
参考文献: |
1. Dueweke TJ, et al. U-90152, a potent inhibitor of human immunodeficiency virus type 1 replication. Antimicrob Agents Chemother. 1993 May;37(5):1127-31. 2. Mayland Chang, et al. Metabolism of the HIV-1 Reverse Transcriptase Inhibitor Delavirdine In Mice. Research Article |
溶解性: |
DMSO : ≥ 40.3 mg/mL (72.92 mM) |
保存条件: |
2-8℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
1.809 ml |
9.047 ml |
18.094 ml |
5 mM |
0.362 ml |
1.809 ml |
3.619 ml |
10 mM |
0.181 ml |
0.905 ml |
1.809 ml |
50 mM |
0.036 ml |
0.181 ml |
0.362 ml |
|
注意: |
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