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/ Rilpivirine/利匹韦林

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

货号：A112484 同义名： R278474; TMC278

Rilpivirine是一种非核苷类逆转录酶抑制剂（NNRTI），具有抗 HIV 效果。

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

货号：A112484 标准纯度： {[allProObj[0].p_purity_real_show]}
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Rilpivirine/利匹韦林 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/利匹韦林 细胞实验

Cell Line
Concentration Treated Time Description References
Xenopus laevis oocytes 20 µM 1 hour To assess the accumulation of rilpivirine in oocytes expressing various transporters, results showed rilpivirine was not significantly transported by any of the tested transporters Antimicrob Agents Chemother. 2013 Nov;57(11):5612-8.
Human monocyte-derived macrophages (MDM) 0.2–200 µM (based on RPV concentration) 12 hours Evaluate the effects of EuCF-RPV particles on MDM cell vitality. At the highest concentration tested, 200 μM, NRPV and EuCF-RPV less effected cell vitality than native RPV (82.9%, 56.9% and 37.9%, respectively). Biomaterials. 2018 Dec;185:174-193.
Human preadipocytes 10 µM 15 days Rilpivirine at 10 μM significantly impaired adipocyte differentiation and induced the expression and release of proinflammatory cytokines. Antimicrob Agents Chemother. 2012 Jun;56(6):3369-75.
Human preadipocytes 4 µM 15 days Rilpivirine at 4 μM significantly impaired adipocyte differentiation, but the effect was milder than that of efavirenz at the same concentration. Antimicrob Agents Chemother. 2012 Jun;56(6):3369-75.
Human preadipocytes 0.01-10 µM 15 days Rilpivirine had no effect on the acquisition of adipocyte morphology at concentrations up to 2 μM, but significantly impaired adipocyte differentiation at 4 μM and 10 μM. Antimicrob Agents Chemother. 2012 Jun;56(6):3369-75.
CEM-CD4+ T cells 0.1–1000 nM 2 hours Determine the EC50 of M3RPV and RPV in CEM-CD4+ T cells. Results showed that M3RPV had a 6.8-fold higher EC50 compared to RPV. J Control Release. 2019 Oct;311-312:201-211.
Human monocyte-derived macrophages (MDMs) 20 µM 24 hours To evaluate the uptake and antiviral efficacy of LBNP-RPV-CCR5 in MDMs. Results showed that LBNP-RPV-CCR5 had a 3-fold higher uptake at 12 h compared to LBNP-RPV and entered cells via CCR5 receptor-mediated pathways. Nat Commun. 2025 Jan 8;16(1):513.
U-937 0.625-40 µM 24, 48, or 72 hours Evaluate the inhibitory effect of Rilpivirine on U-937 cell proliferation, showing GI50 values of 4.12-12.39 µM Cancers (Basel). 2023 Feb 7;15(4):1044.
K-562 0.625-40 µM 24, 48, or 72 hours Evaluate the inhibitory effect of Rilpivirine on K-562 cell proliferation, showing GI50 values of 4.12-12.39 µM Cancers (Basel). 2023 Feb 7;15(4):1044.
NB4 0.625-40 µM 24, 48, or 72 hours Evaluate the inhibitory effect of Rilpivirine on NB4 cell proliferation, showing GI50 values of 4.12-12.39 µM Cancers (Basel). 2023 Feb 7;15(4):1044.
HL-60 0.625-40 µM 24, 48, or 72 hours Evaluate the inhibitory effect of Rilpivirine on HL-60 cell proliferation, showing GI50 values of 4.12-12.39 µM Cancers (Basel). 2023 Feb 7;15(4):1044.
LX-2 cells 1-8 µM 24-48 hours To evaluate the effect of RPV on autophagy in TGF-β-activated LX-2 cells. Results showed that RPV enhanced the expression of autophagy markers, increased autophagosome content and lysosomal mass. Cell Death Dis. 2022 Apr 20;13(4):385.
SLC22A1-overexpressing KCL22 cells 20 µM 30 minutes To assess the accumulation of rilpivirine in SLC22A1-overexpressing cells, results showed significantly higher accumulation in SLC22A1-overexpressing cells compared to control cells Antimicrob Agents Chemother. 2013 Nov;57(11):5612-8.
CEMVBL100 cells 20 µM 30 minutes To assess the accumulation of rilpivirine in ABCB1-overexpressing cells, results showed no significant difference in accumulation between CEMVBL100 and CEM cells Antimicrob Agents Chemother. 2013 Nov;57(11):5612-8.
Primary human hepatic stellate cells 1-8 µM 48 hours To verify whether RPV also enhances autophagy in non-immortalized primary HSC. Results showed that RPV similarly enhanced autophagy in primary HSC. Cell Death Dis. 2022 Apr 20;13(4):385.
Caco-2 cell monolayers 20 µM 60 minutes To assess the permeability of rilpivirine in Caco-2 cell monolayers, results showed significantly higher transport in the B-to-A direction than A-to-B direction, but ABCB1 inhibitor tariquidar did not significantly alter permeability Antimicrob Agents Chemother. 2013 Nov;57(11):5612-8.
CD4+ T cells 100 µM 8 hours Assessed uptake and cell vitality of RPV-NC in CD4+ T cells, showing no cytotoxicity and maximum uptake at 8 hours (8 μg/10^6 cells) Biomaterials. 2020 Feb;231:119669.
Human monocyte-derived macrophages (MDM) 100 µM 8 hours Assessed uptake and cell vitality of RPV-NC in macrophages, showing no cytotoxicity and maximum uptake at 6 hours (60 μg/10^6 cells) Biomaterials. 2020 Feb;231:119669.
Human monocyte-derived macrophages (MDM) 25 µM 8 hours Assess uptake and retention of EuCF-RPV particles in MDM. At 8 hours, cells contained 14 μg/106 cells of RPV, 9.5 μg iron/106 cells and 2.9 μg cobalt/106 cells. Biomaterials. 2018 Dec;185:174-193.

Rilpivirine/利匹韦林 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice HL-60 xenograft model Oral 200 mg/kg Once daily for 15 days Evaluate the anti-leukaemic efficacy of Rilpivirine in the HL-60 xenograft model, showing significant inhibition of tumour growth Cancers (Basel). 2023 Feb 7;15(4):1044.
Humanized mice (hu mice) HIV-1-infected humanized mouse model Tail vein injection 25 mg/kg Single dose, lasting 14 days To evaluate the antiviral efficacy and biodistribution of LBNP-RPV-CCR5 in HIV-1-infected humanized mice. Results showed that LBNP-RPV-CCR5 specifically accumulated in the spleen and enhanced brain delivery via FUS-mediated BBB disruption. Nat Commun. 2025 Jan 8;16(1):513.
Male Balb/cJ mice Healthy mice Intravenous injection 45 mg/kg Single injection, observed up to 28 days Evaluate tissue biodistribution and antiretroviral activities of 111InEuCF-PCL/RPV particles in mice. Particles accumulated in liver, spleen, and lymph nodes and were validated by MRI and SPECT/CT imaging. Biomaterials. 2018 Dec;185:174-193.
C57BL/6J mice HFD-induced NAFLD model and CCl4-induced hepatotoxicity model Oral 5 mg/kg/day Once daily for 12 weeks (NAFLD model) or 4 weeks (CCl4 model) To evaluate the hepatoprotective effect of RPV in chronic liver injury models and its impact on autophagy. Results showed that RPV enhanced hepatic autophagy and attenuated liver injury. Cell Death Dis. 2022 Apr 20;13(4):385.

Rilpivirine/利匹韦林 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/利匹韦林 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/利匹韦林 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/利匹韦林 技术信息

CAS号500287-72-9
分子式C22H18N6
分子量 366.42
SMILES Code N#CC1=CC=C(NC2=NC=CC(NC3=C(C)C=C(/C=C/C#N)C=C3C)=N2)C=C1
MDL No. MFCD11046372
别名 R278474; TMC278; DB08864
运输蓝冰
InChI Key YIBOMRUWOWDFLG-ONEGZZNKSA-N
Pubchem ID 6451164
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: Rilpivirine | R278474;TMC278;DB08864 | HIV | Reverse Transcriptase | NNRTI | AmBeed-信号通路专用抑制剂 | Rilpivirine/利匹韦林 纯度/质量文件 | Rilpivirine/利匹韦林 生物活性 | Rilpivirine/利匹韦林 临床数据 | Rilpivirine/利匹韦林 参考文献 | Rilpivirine/利匹韦林 实验方案 | Rilpivirine/利匹韦林 技术信息

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