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抑制剂/激活剂

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凋亡与自噬

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Rilpivirine 利匹韦林; R278474; TMC278; DB08864

Rilpivirine (R278474) 是一种有效和特异性的二芳基嘧啶 (DAPY) 非核苷逆转录酶抑制剂 (NNRTI)。Rilpivirine 对野生型 HIV (EC50=0.4 nM) 和突变体 (EC50=0.1-2.0 nM) 具有很高的抗病毒活性。Rilpivirine 对 HIV 耐药性的形成产生了高度的遗传障碍。

货号：
TK0542
规格：

1mg

2mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	500287-72-9
生物活性	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.
分子式	C22H18N6
分子量	366.42
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 50 mg/mL (136.46 mM; Need ultrasonic)
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.
体外研究	R278474 is active against wild-type HIV-1 (EC50=0.4 nM) and all single and double mutants tested (EC50=0.1-2.0 nM). R278474 (10-5000 nM; 30 d) does not observe the sign of wild-type HIV-1 breakthrough at 1 μM within 30 days. R278474 inhibits 81% of clinical isolates (about 1200 recombinant clinical isolates) at a 50% inhibitory concentration (EC50) less than 1 nM, and inhibits 94% at EC50 less than 10 nM. TMC278 shows subnanomolar EC50s against wild-type HIV-1 group M isolates (0.07-1.01 nM) and nanomolar EC50s against group O isolates (2.88-8.45 nM) in MT4 T-cells.
文献	•Int J Antimicrob Agents. 2019 Dec;54(6):814-819. •Sci Rep. 2015 Oct 29;5:15806. •PLoS One. 2021 Mar 10;16(3):e0248139. •Biol Pharm Bull. 2016;39(3):450-4. •Faculty of Pharmacy in Hradec Králové Department of Pharmacological and Toxicology. University of Oxford. 2019 Jul.
纯度及产品资料	98%

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