Delavirdine mesylate

Research use only, not for human use.

A potent HIV-1 reverse transcriptase inhibitor with IC50 of 0.26 uM for recombinant HIV-1 RT.

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) 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).

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.

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).

U 90152

Microbiology/Virology

HIV

HIV

Infection

HIV Infection

147221-93-0

552.6668

C23H32N6O6S2

>98% (HPLC)

DMSO: ≥ 40.3 mg/mL

O=C(N1CCN(C2=NC=CC=C2NC(C)C)CC1)C(N3)=CC4=C3C=CC(NS(=O)(C)=O)=C4.CS(=O)(O)=O

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

(-20℃)

With Ice Pack

≥ 2 years