Delavirdine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的 HIV-1 逆转录酶抑制剂，对于重组 HIV-1 RT 的 IC50 为 0.26 uM。

A potent HIV-1 reverse transcriptase inhibitor with IC50 of 0.26 uM for recombinant HIV-1 RT; exhibits IC50>440 uM for DNA polymerases α and δ; blocks the replication in peripheral blood lymphocytes of 25 primary HIV-1 isolates and has low cellular cytotoxicity; retains significant activity against mutant RTs (K103N, Y181C).HIV Infection Approved(In Vitro):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 IC50 value of 0.26 μM, and it inhibits Y181C-substituted RT and K103N-substituted RT with IC50 values of 8.32 uM and 7.7 uM, respectively.(In Vivo):Delavirdine (U 90152) (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).

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 IC50 value of 0.26 μM, and it inhibits Y181C-substituted RT and K103N-substituted RT with IC50 values of 8.32 uM and 7.7 uM, respectively.

Delavirdine (U 90152) (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).

U 90152 | BHAP-U 90152

Microbiology/Virology

HIV

HIV

Infection

HIV Infection

136817-59-9

456.5611

C22H28N6O3S

>98% (HPLC)

10 mM in DMSO

CC(C)NC1=C(N=CC=C1)N2CCN(CC2)C(=O)C3=CC4=C(N3)C=CC(=C4)NS(=O)(=O)C

Methanesulfonamide, N-[2-[[4-[3-[(1-methylethyl)amino]-2-pyridinyl]-1-piperazinyl]carbonyl]-1H-indol-5-yl]-

(-20℃)

With Ice Pack

≥ 2 years