Etravirine-R165335-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEtravirineCat. No.: HY-90005CAS No.: 269055-15-4Synonyms: R165335; TMC125分式: CHBrNO分量: 435.28作靶點: Reverse Transcriptase; HIV作通路: Anti-infection儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO

2、: 50 mg/mL (114.87 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.74 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.74 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Etravirine種核苷逆轉(zhuǎn)錄酶抑制劑

3、(NNRTI)，于治療 HIV。體外研究 TMC125 is highly active against wild-type HIV-1 (50% effective concentration EC50=1.4 to 4.8 nM) andshows some activity against HIV-2 (EC50=3.5 M). TMC125 also inhibits a series of HIV-1 group M subtypesand circulating recombinant forms and a group O virus. TMC125 has activity f

4、or 19 viruses with EC50 of 5nM 1.體內(nèi)研究 Etravirine has a high genetic barrier to the development of resistance. In phase IIb trials in treatment-experienced patients, including those infected with virus resistant to NNRTIs and protease inhibitors (PIs),TMC125 is active against HIV resistant to current

5、ly available NNRTIs, with a similar tolerability profile to thatof the control group 2.戶使本產(chǎn)品發(fā)表的科研獻 Antimicrob Agents Chemother. 2015 Dec;59(12):7666-7670. Sci Rep. 2015 Oct 29;5:15806. Biol Pharm Bull. 2016;39(3):450-4.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Andries, K.

6、, et al. TMC125, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reversetranscriptase inhibitor-resistant human immunodeficiency virus type 1. Antimicrob Agents Chemother, 2004. 48(12): p. 4682. Lazzarin, A., et al. Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in DUET-2: 24-weekresults from a randomised, double-blind, placebo-controlled trial. Lancet, 2007. 370(9581): p. 39-48.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use onl