Delavirdine (mesylate)

CAS No. : 147221-93-0

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

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Cat. No. : HY-10571A
M.Wt: 552.67
Formula: C23H32N6O6S2
Purity: >98 %
Solubility: DMSO : ≥ 40.3 mg/mL (72.92 mM)
Introduction of 147221-93-0 :

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

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