For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>Delavirdine(U 90152) is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI).<br>IC50 Value: 0.26 uM (Recombinant HIV-1 RT) [1]<br>Target: HIV-1 reverse transcriptase; NNRTI<br>in vitro: U-90152 [1-(5-methanesulfonamido-1H-indol-2-yl-carbonyl)-4-[3-(1-methyl eth yl-amino)pyridinyl]piperazine], which inhibited recombinant HIV-1 RT at a 50% inhibitory concentration (IC50) of 0.26 microM (compared with IC50s of > 440 microM for DNA polymerases alpha and delta). U-90152 blocked the replication in peripheral blood lymphocytes of 25 primary HIV-1 isolates, including variants that were highly resistant to 3/’-azido-2/’,3/’-dideoxythymidine (AZT) or 2/’,3/’-dideoxyinosine, with a mean 50% effective dose of 0.066 +/- 0.137 microM. U-90152 had low cellular cytotoxicity, causing less than 8% reduction in peripheral blood lymphocyte viability at 100 microM. In experiments assessing inhibition of the spread of HIV-1IIIB in cell cultures, U-90152 was much more effective than AZT. When approximately 500 HIV-1IIIB-infected MT-4 cells were mixed 1:1,000 with uninfected cells, 3 microM AZT delayed the evidence of rapid viral growth for 7 days. In contrast, 3 microM U-90152 totally prevented the spread of HIV-1, and death and/or dilution of the original inoculum of infected cells prevented renewed viral growth after U-90152 was removed at day 24 [1]. Asdelavirdine concentration was increased from 0 to 100 microM, the K(M) for diclofenac metabolism rose from 4.5+/-0.5 to 21+/-6 microM, and V(max) declined from 4.2+/-0.1 to 0.54+/-0.08 nmol/min/mg of protein, characteristic of mixed-type inhibition [2].<br>in vivo: The mean values (+/- standard deviations) for the maximum concentration in serum (C(max)) of ritonavir, the area under the concentration-time curve from 0 to 12 h (AUC(0-12)), and the minimum concentration in serum (C(min)) of ritonavir before the addition of delavirdine were 14.8 +/- 6.7 micro M, 94 +/- 36 micro M. h, and 3.6 +/- 2.1 micro M, respectively. These same parameters were increased to 24.6 +/- 13.9 micro M, 154 +/- 83 micro M. h, and 6.52 +/- 4.85 micro M, respectively, after the addition of delavirdine(P is <0.05 for all comparisons). Delavirdine pharmacokinetic parameters in the presence of ritonavir included a C(max) of 23 +/- 16 micro M, an AUC(0-8) of 114 +/- 75 micro M. h, and a C(min) of 9.1 +/- 7.5 micro M [3].<br>Toxicity:<br>Clinical trial: Quality of Life of HIV-infected Participants Switched to Raltegravir Versus Other Antiretroviral Regimens. Phase 4<br></p>
| Catalog Number | I001420 |
| CAS Number | 136817-59-9 |
| Synonyms | N-[2-[4-[3-(propan-2-ylamino)pyridin-2-yl]piperazine-1-carbonyl]-1H-indol-5-yl]methanesulfonamide |
| Molecular Formula | C22H28N6O3S |
| Purity | ≥95% |
| Target | Reverse Transcriptase |
| Solubility | 10mM in DMSO |
| Storage | Store at -20C |
| IC50 | 0.26 uM (Recombinant HIV-1 RT) [1] |
| Reference | </br>1:Effect of six antiretroviral drugs (delavirdine, stavudine, lamivudine, nelfinavir, amprenavir and lopinavir/ritonavir in association) on albino pregnant rats (Rattus norvegicus Albinus, Rodentia, Mammalia): biological assay. Nakamura MU, Araujo Júnior E, Simões JM, Oliveria RM, Kulay LJ.Ceska Gynekol. 2014 Aug;79(4):295-304. PMID: 25398151 </br>2:Solid lipid nanoparticles comprising internal Compritol 888 ATO, tripalmitin and cacao butter for encapsulating and releasing stavudine, delavirdine and saquinavir. Kuo YC, Chung CY.Colloids Surf B Biointerfaces. 2011 Dec 1;88(2):682-90. doi: 10.1016/j.colsurfb.2011.07.060. Epub 2011 Aug 6. PMID: 21865017 </br>3:Design and synthesis of dual inhibitors of HIV reverse transcriptase and integrase: introducing a diketoacid functionality into delavirdine. Wang Z, Vince R.Bioorg Med Chem. 2008 Apr 1;16(7):3587-95. doi: 10.1016/j.bmc.2008.02.007. Epub 2008 Feb 8. PMID: 18314335 </br>4:Multiple-Dose Pharmacokinetics of Delavirdine Mesylate and Didanosine in HIV-Infected Patients. Morse GD, Cohn SE, Shelton MJ, Greisberger C, Cox SR, Della-Coletta AA, Freimuth WW, Reichman RC.Clin Drug Investig. 2003;23(5):323-8. PMID: 17535044 </br>5:Effect of Food on the Steady-State Pharmacokinetics of Delavirdine in Patients with HIV Infection. Morse GD, Fischl MA, Shelton MJ, Cox SR, Thompson L, Della-Coletta AA, Freimuth WW.Clin Drug Investig. 2003;23(4):255-61. PMID: 17535038 </br>6:Transport of stavudine, delavirdine, and saquinavir across the blood-brain barrier by polybutylcyanoacrylate, methylmethacrylate-sulfopropylmethacrylate, and solid lipid nanoparticles. Kuo YC, Su FL.Int J Pharm. 2007 Aug 1;340(1-2):143-52. Epub 2007 Mar 12. PMID: 17418986 </br>7:Interactions between buprenorphine and antiretrovirals. I. The nonnucleoside reverse-transcriptase inhibitors efavirenz and delavirdine. McCance-Katz EF, Moody DE, Morse GD, Friedland G, Pade P, Baker J, Alvanzo A, Smith P, Ogundele A, Jatlow P, Rainey PM.Clin Infect Dis. 2006 Dec 15;43 Suppl 4:S224-34. PMID: 17109309 </br>8:Drug interactions between opioids and antiretroviral medications: interaction between methadone, LAAM, and delavirdine. McCance-Katz EF, Rainey PM, Smith P, Morse GD, Friedland G, Boyarsky B, Gourevitch M, Jatlow P.Am J Addict. 2006 Jan-Feb;15(1):23-34. PMID: 16449090 </br>9:Population pharmacokinetics of delavirdine and N-delavirdine in HIV-infected individuals. Smith PF, Dicenzo R, Forrest A, Shelton M, Friedland G, Para M, Pollard R, Fischl M, DiFrancesco R, Morse GD.Clin Pharmacokinet. 2005;44(1):99-109. PMID: 15634033 </br>10:Effects of the G190A substitution of HIV reverse transcriptase on phenotypic susceptibility of patient isolates to delavirdine. Uhlmann EJ, Tebas P, Storch GA, Powderly WG, Lie YS, Whitcomb JM, Hellmann NS, Arens MQ.J Clin Virol. 2004 Nov;31(3):198-203. PMID: 15465412 |
