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利匹韦林 /Rilpivirine {[allProObj[0].p_purity_real_show]}

货号:A112484 同义名: R278474;TMC278

Rilpivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) with anti-HIV effect.

Rilpivirine 化学结构 CAS号:500287-72-9
Rilpivirine 化学结构
CAS号:500287-72-9
Rilpivirine 3D分子结构
CAS号:500287-72-9
Rilpivirine 化学结构 CAS号:500287-72-9
Rilpivirine 3D分子结构 CAS号:500287-72-9
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Rilpivirine 纯度/质量文件 产品仅供科研

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Rilpivirine 生物活性

描述 Rilpivirine is a diarylpyrimidine derivative that functions as a non-nucleoside reverse transcriptase inhibitor (NNRTI) for the treatment of HIV-1 infection. It demonstrated more pronounced activity against wild-type HIV-1 (EC50 = 0.4 nM) and all single and double mutants as compared to other NNRTIs, such as nevirapine, efavirenz, TMC120, and TMC125. Rilpivirine at 1 μM showed no sign of virus breakthrough for wild-type HIV-1 within 30 days. Compared to the E-isomer of rilpivirine, the Z-isomer exhibited relatively high potency against wild-type HIV-1 with an EC50 value of 0.6 nM, but showed five times less activity against single and double mutants. Rilpivirine inhibited 81% of the 1200 recombinant clinical isolates collected from HIV-infected patients with an EC50 value less than 1 nM. The IC50 values of rilpivirine for the inhibition of CYP450 isoforms 3A4, 2C9, and 2D6 were 4.6, 5.0, and >10 μM, respectively. The pharmacokinetic studies after the i.v. administration of rilpivirine showed that the elimination half-life was 4.4 h in rat and 31h in dog. The exposure (AUCinf) were 3.1 μg h/mL (i.v. dose of 4 mg/kg) in rat, 8.7 μg h/mL (i.v. dose of 1.25 mg/kg) in dog, 1.4 μg h/mL (i.v. dose of 1.25 mg/kg) in monkey, and 44 μg h/mL (i.v. dose of 1.25 mg/kg) in rabbit.
作用机制 Rilpivirine is a NNRTI that shows potent activity against wild-type and mutant HIV-1 strains. The improved activity in comparison to other NNRTIs may involve a specific interaction of the cyano group in wing I with the indole ring of Trp229.

Rilpivirine 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
human MT4 cells Function assay 72 h Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay, EC50=0.0037 μM 23137340
human PBMC cells Function assay Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG001 infected in human PBMC cells by cell based assay, EC50=0.00026 μM 19933797
human TZM-bl cells Cytotoxicity assay 4 days Cytotoxicity against human TZM-bl cells after 4 days by XTT assay, CC50=19.4 μM 22856541
MT2 cells Cytotoxicity assay Cytotoxicity in human MT2 cells assessed as inhibition of cell growth, CC50=8 μM 23298809

Rilpivirine 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02491242 - Completed - Spain ... 展开 >> Ramon y Cajal Hospital Madrid, Spain, 28034 收起 <<
NCT02605954 HIV-1 Infection Phase 3 Completed - -
NCT03631732 HIV-1 Infection Phase 3 Recruiting August 2020 -

Rilpivirine 参考文献

[1]Azijn H, Tirry I, 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.

[2]Janssen PA, Lewi PJ, 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):1901-9.

Rilpivirine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.73mL

0.55mL

0.27mL

13.65mL

2.73mL

1.36mL

27.29mL

5.46mL

2.73mL

Rilpivirine 技术信息

CAS号500287-72-9
分子式C22H18N6
分子量 366.42
别名 R278474;TMC278;DB08864
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

溶解度

DMSO: 50 mg/mL(136.46 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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