Rilpivirine-R278474-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERilpivirineCat. No.: HY-10574CAS No.: 500287-72-9Synonyms: R278474; TMC278; DB08864分式: CHN分量: 366.42作靶點(diǎn): HIV; Reverse Transcriptase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(shí)

2、驗(yàn) DMSO : 50 mg/mL (136.46 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 3 mg/mL (8.19 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 3 mg/mL (8.19 mM); Suspended solution; Need ultrasonic1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請依序

3、添加每種溶劑： 10% DMSO 90% corn oilSolubility: 3 mg/mL (8.19 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Rilpivirine (R278474; TMC278)HIV 的核苷逆轉(zhuǎn)錄酶抑制劑。IC50 & Target NNRTIs體外研究 Rilpivirine(TMC278) is a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), activeagainst wild-type and NNRTI-resi

4、stant HIV-1. NNRTIs work by binding to and blocking HIV reversetranscriptase, an HIV enzyme. This prevents HIV from replicating and lowers the amount of HIV in the blood.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Sci Rep. 2015 Oct 29;5:15806. Biol Pharm Bull. 2016;39(3):450-4. Faculty of Pharmacy in Hradec Krlov Department of Pha

5、rmacological and Toxicology. University of Oxford. 2019 Jul.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Singh K, Marchand B, Rai DK, Sharma B, Michailidis E, Ryan EM, Matzek KB, Leslie MD, Hagedorn AN, Li Z, Norden PR, Hachiya A,Parniak MA, Xu HT, Wainberg MA, Sarafianos SG

6、.Biochemical Mechanism of HIV-1 Resistance to Rilpivirine.J Biol Chem. 2012 Sep 6.2. Schafer JJ, Short WR.Rilpivirine, a novel non-nucleoside reverse transcriptase inhibitor for the management of HIV-1 infection: asystematic review.Antivir Ther. 2012 Jul 25.3. Vingerhoets J, Rimsky L, Van Eygen V, N

7、ijs S, Vanveggel S, Boven K, Picchio G.Preexisting mutations in the rilpivirine Phase III trialsECHO and THRIVE: prevalence and impact on virologic response.Antivir Ther. 2012 Sep 6.4. Gomes T, Juurlink DN, Mamdani MM.Comparative adherence to oxybutynin or tolterodine among older patients.Eur J Clin

8、 Pharmacol.2012 Jan;68(1):97-9. Epub 2011 Jun 28.5. Azijn, Hilde et al. TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type andNNRTI-resistant HIV-1.Antimicrobial Agents and Chemotherapy (2010), 54(2), 718-727.McePdfHeightCaution: Product has not been fully validated for medical applications.F