货号	规格	价格	上海	北京	珠海	重庆	武汉
S80747-2mg买3赠1	98.16%	￥240.00 S80747-2mg ￥240.00 现货（买3赠1）	7 7	-	-	-	-
S80747-5mg买3赠1	98.16%	￥400.00 S80747-5mg ￥400.00 现货（买3赠1）	6 6	-	-	-	-
S80747-10mg买3赠1	98.16%	￥640.00 S80747-10mg ￥640.00 现货（买3赠1）	19 >10	-	-	-	-
S80747-50mg买3赠1	98.16%	￥1440.00 S80747-50mg ￥1440.00 现货（买3赠1）	2 2	-	-	-	-
S80747-100mg买3赠1	≥98%	￥2560.00 S80747-100mg ￥2560.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-

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产品描述：

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

靶点：

reverse transcriptase HIV;HIVProtease;ReverseTranscriptase

体内研究：

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.

参考文献：

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)

保存条件：

-20℃

配置溶液浓度参考：

	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

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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