Nevirapine

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Chemical Structure| 129618-40-2 同义名 : 奈韦拉平 ;BI-RG 587;NVP;Brand name: Viramune Viramune XR.;HSDB 7164;BIRG 0587;NSC 641530
CAS号 : 129618-40-2
货号 : A326622
分子式 : C15H14N4O
纯度 : 98%
分子量 : 266.298
MDL号 : MFCD00866928
存储条件：

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：
生物活性
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].
细胞研究
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
实验方案
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
参考文献

[1]Mangiacasale R, Pittoggi C, et al. Exposure of normal and transformed cells to nevirapine, a reverse transcriptase inhibitor, reduces cell growth and promotes differentiation. Oncogene. 2003 May 8;22(18):2750-61.

[2]Erickson DA, Mather G, et al. Characterization of the in vitro biotransformation of the HIV-1 reverse transcriptase inhibitor nevirapine by human hepatic cytochromes P-450. Drug Metab Dispos. 1999 Dec;27(12):1488-95.

[3]Erickson DA, Mather G, Trager WF, Levy RH, Keirns JJ. Characterization of the in vitro biotransformation of the HIV-1 reverse transcriptase inhibitor nevirapine by human hepatic cytochromes P-450. Drug Metab Dispos. 1999 Dec;27(12):1488-95

[4]Dong JJ, Zhou Y, Liu YT, Zhang ZW, Zhou XJ, Wang HJ, Liao L. In vitro evaluation of the therapeutic potential of nevirapine in treatment of human thyroid anaplastic carcinoma. Mol Cell Endocrinol. 2013 May 6;370(1-2):113-8

[5]Milinkovic A, Martínez E. Nevirapine in the treatment of HIV. Expert Rev Anti Infect Ther. 2004 Jun;2(3):367-73

[6]Onasanwo SA, Adeyemi JA, Latinwo GG, Faborode SO, Mishra V. Evaluation of anti-ulcerogenic and ulcer-healing activities of nevirapine in rats. Afr J Med Med Sci. 2015 Sep;44(3):251-9

[7]Bardsley-Elliot A, Perry CM. Nevirapine: a review of its use in the prevention and treatment of paediatric HIV infection. Paediatr Drugs. 2000 Sep-Oct;2(5):373-407