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| 描述 | Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM. Nevirapine itself is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki=270 μM)[3]. At all doses (100, 200, 350, 500 μM) tested, nevirapine significantly inhibited cell proliferation after 48 h treatment. At high dose (500 μM), nevirapine significantly increased the percentage of apoptotic cells compared with control (P<0.01). At lower doses (200 μM and 350 μM), nevirapine did not induce cell apoptosis, but up-regulated NIS and THSR mRNA expression in a dose-dependent manner[4]. Nevirapine also has an important role in preventing mother-to-child transmission of HIV. Nevirapine interacts with cytochrome P450 enzymes both as a substrate and as an inducer[5]. Nevirapine (9 mg/kg, 18 mg/kg and 36 mg/kg) showed significant (P < 0.05) reduction in ulcer severity score and ulcer index as compared to the control in the models,.with corresponding increase in percentage inhibition[6]. Nevirapine inhibits replication of multiple HIV-1 strains and clinical isolates in cultured human T cells, but has no activity against other retroviral RTs (including HIV-2 RT) or endogenous human DNA polymerases[7]. |
| Administration | Dosage | Frequency | Description | References | ||
| Oreochromis mossambicus | Oreochromis mossambicus | Water exposure | 1.48 mg/L and 3.74 mg/L | 30 days | The study investigated the effects of nevirapine and its mixture with antibiotics on the gonads of Oreochromis mossambicus. Female fish exposed to 3.74 mg/L nevirapine and its mixture showed significantly higher ovary indices, with increased vitellogenic oocyte atresia and vacuolation of the interstitial tissue observed in the ovaries. | Chemosphere. 2021 Jul;274:129900 |
| Mice | LDLr −/− and hA-I transgenic mice | Oral | 20 mg/kg | Once daily for 12 weeks | To study the effects of nevirapine on HDL cholesterol levels and reverse cholesterol transport, results showed that nevirapine significantly increased HDL cholesterol levels at week 4, but no significant difference was observed at weeks 8 and 12 compared to control | Atherosclerosis. 2009 Jun;204(2):418-23 |
| Mice | LINE-1a mice | Oral | 100 μg | Once daily for 4 weeks | Nevirapine treatment did not significantly affect the progression of ataxia in LINE-1a mice. | Neuron. 2022 Oct 19;110(20):3278-3287.e8 |
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
| 293T cells | Function assay | Inhibition of wild type HIV1 reverse transcriptase in 293T cells, IC50=0.06 μM | 16527484 | ||
| CEM-SS cells | Function assay | Antiviral activity against HIV1 RF in CEM-SS cells assessed as inhibition of virus-induced cytopathic effect by XTT assay, EC50=1.5 nM | 18222088 | ||
| HeLa cells | Function assay | Antiviral activity against wild type HIV1 in HeLa cells by MAGI assay, IC50=0.053 μM | 18665583 | ||
| human C1866 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human C1866 cells after 72 hrs by MTT assay, EC50=0.04943 μM | 21194939 | |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
3.76mL 0.75mL 0.38mL |
18.78mL 3.76mL 1.88mL |
37.55mL 7.51mL 3.76mL |
|
| CAS号 | 129618-40-2 |
| 分子式 | C15H14N4O |
| 分子量 | 266.3 |
| SMILES Code | O=C1C2=CC=CN=C2N(C3CC3)C4=NC=CC(C)=C4N1 |
| MDL No. | MFCD00866928 |
| 别名 | 奈韦拉平 ;BI-RG 587; HSDB 7164; BIRG 0587; NSC 641530 |
| 运输 | 蓝冰 |
| InChI Key | NQDJXKOVJZTUJA-UHFFFAOYSA-N |
| Pubchem ID | 4463 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, room temperature |
| 溶解方案 |
DMSO: 15 mg/mL(56.33 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 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
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