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Rilpivirine 98%

Rilpivirine

源葉(MedMol)
S80747
500287-72-9
C22H18N6
366.42
品牌 貨號(hào) 產(chǎn)品規(guī)格 價(jià)格(RMB) 庫(kù)存(上海) 北京 武漢 南京 購(gòu)買數(shù)量
源葉(MedMol) S80747-2mg 98% ¥240.00元 2 - - -
源葉(MedMol) S80747-5mg 98% ¥400.00元 預(yù)計(jì)交期:2-3天 - - -
源葉(MedMol) S80747-10mg 98% ¥640.00元 >10 - - -
源葉(MedMol) S80747-50mg 98% ¥1440.00元 7 - - -
源葉(MedMol) S80747-100mg 98% ¥2560.00元 預(yù)計(jì)交期:2-3天 - - -
產(chǎn)品介紹 參考文獻(xiàn) 質(zhì)檢證書(COA) 摩爾濃度計(jì)算器 相關(guān)產(chǎn)品

產(chǎn)品介紹

Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV
產(chǎn)品描述: Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV
靶點(diǎn): reverse transcriptase HIV;HIVProtease;ReverseTranscriptase
體內(nèi)研究:
R278474 (10-160 mg/kg; p.o. for 1 month) does not produce abnormal effects in rat, apart from liver weight increase and species-specific thyroid hypertrophy, both at the higher dose levels. R278474 (i.v.) exhibits elimination half-life ranges from 4.4 h in rat to 31 h in dog, and exposure (AUCinf) amounts to 3.1 μg?h/mL (4 mg/kg) in rat, 8.7 μg?h/mL (1.25 mg/kg) in dog, 1.4 μg?h/mL (1.25 mg/ kg) in monkey, and 44?μg h/mL (1.25 mg/kg) in rabbit. R278474 (p.o.) exhibits half-life ranges between 2.8 h in rat and 39 h in dog, and oral bioavailability of 32% and 31% in rat and dog.
參考文獻(xiàn):
1. Janssen PAJ, et, al. In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine). J Med Chem. 2005 Mar 24;48(6):1 2. Azijn H, et, al. TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. Antimicrob Agents Chemother. 2010 Feb;54(2):718-27.
溶解性: DMSO  :  50  mg/mL  (136.46  mM;  Need  ultrasonic)
保存條件: -20℃
配置溶液濃度參考:
1mg 5mg 10mg
1 mM 2.729 ml 13.646 ml 27.291 ml
5 mM 0.546 ml 2.729 ml 5.458 ml
10 mM 0.273 ml 1.365 ml 2.729 ml
50 mM 0.055 ml 0.273 ml 0.546 ml
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