Delavirdine  (Synonyms: U 90152; BHAP-U 90152)

Delavirdine (U 90152) is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine 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 is an inhibitor of HIV-1 replication and can can be used for the study of AIDs^[1].

IC50: 0.26 μM (HIV-1 RT); 440 μM (DNA polymerase α); >550 μM (DNA polymerase δ)^[1]

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^[1].
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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

456.56

C₂₂H₂₈N₆O₃S

136817-59-9

O=S(NC1=CC=C(NC(C(N2CCN(C3=C(NC(C)C)C=CC=N3)CC2)=O)=C4)C4=C1)(C)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [2]. Mayland Chang, et al. Metabolism of the HIV-1 Reverse Transcriptase Inhibitor Delavirdine In Mice. Research Article