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编 号:F171263
分子式:C23H32N6O6S2
分子量:552.67
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10mM*1mL in DMSO
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5mg
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10mg
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50mg
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100mg
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200mg
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生物活性:
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.

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).

体外研究:
Delavirdine has an 50% cytotoxicity at concentrations >100 μM in H9 and PBMC cultures.Delavirdine has low cellular cytotoxicity, causing less than 8% reduction in peripheral blood lymphocyte viability at 100 μM.Delavirdine inhibits HIV-1 reverse transcriptase (RT) wild type with an IC50value of 0.26?μM, and it inhibits Y181C-substituted RT and K103N-substituted RT with IC50values of 8.32 uM and 7.7 uM, respectively.
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