| Description | Nevirapine (NVP) is a benzodiazepine non-nucleoside reverse transcriptase inhibitor. In combination with other antiretroviral drugs, nevirapine reduces HIV viral loads and increases CD4 counts, thereby retarding or preventing the damage to the immune system and reducing the risk of developing AIDS. |
| In vitro | Nevirapine（NVP）各类动物体内的代谢情况如下：除雄性大鼠以外所有动物的粪便主要代谢物之一是3- OHNVP.所有雄性动物和雌性小鼠,狗和猴的主要代谢物之一是4- CANVP.大鼠胆汁的主要代谢物是4- CANVP和12-OHNVP葡糖苷酸. |
| In vivo | Nevirapine（NVP）本身仅为CYP3A4的抑制剂,且抑制浓度远高于治疗相关（Ki：270 μM）的浓度。 作为非核苷逆转录酶抑制剂,Nevirapine可有效抑制逆转录病毒来源的逆转录酶。Nevirapine也可有效抑制鼠和人细胞系中的内源性逆转录。Nevirapine可挽救急性髓系白血病(AML)细胞系和AML患者的原发细胞中存在的分化阻滞,如形态学、功能和免疫表型分析所示。 Nevirapine使RNA酶H的切割特异性发生改变,导致Nevirapine诱发的核糖核酸酶H活性超过切割特异性变化的预期。Nevirapine是HIV-1逆转录酶（RT）的高特异性抑制剂,在酶分析中IC50为84 nM,在细胞培养物中抗HIV-1复制的IC50为40 nM。 |
| Cell experiments | FRO cells are seeded into 96-well culture plates at 10,000 cells/well. Cells are treated with different doses of nevirapine (0, 100, 200, 350 and 500 μM) for 48 h. MTT dye (5 mg/mL) is added to each well for additional 4 h, and the reaction is then stopped by the addition of DMSO. Optical density is measured at 490 nm on a multi-well plate reader[2]. |
| Target activity | HIV-1:270 μM(ki) |
| Synonyms | NSC 641530, 奈韦拉平, BI-RG 587, 奈伟拉平, NVP |
| molecular weight | 266.3 |
| Molecular formula | C15H14N4O |
| CAS | 129618-40-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 18.33 mg/mL (68.84 mM), Sonication is recommended. |
| References | 1. Erickson DA, et al. Drug Metab Dispos, 1999, 27(12), 1488-1495. 2. Mangiacasale R, et al. Oncogene, 2003, 22(18), 2750-2761. 3. Grob PM, et al. AIDS Res Hum Retroviruses, 1992, 8(2), 145-152. 4. Palaniappan C, et al. J Biol Chem, 1995, 270(9), 4861-4869. 5. Riska PS, et al. Drug Metab Dispos, 1999, 27(12), 1434-1447. 6. Onasanwo SA, et al. Evaluation of anti-ulcerogenic and ulcer-healing activities of nevirapine in rats. Afr J Med Med Sci. 2015 Sep;44(3):251-9. 7. Wu Y, Yang J, Duan C, et al. Simultaneous determination of antiretroviral drugs in human hair with liquid chromatography-electrospray ionization-tandem mass spectrometry[J]. Journal of Chromatography B. 2018 Apr 15;1083:209-221. 8. Tan S, Li W, Li Z, et al. A Novel CXCR4 Targeting Protein SDF-1/54 as an HIV-1 Entry Inhibitor. Viruses. 2019, 11(9): 874. 9. Tan S, Li J Q, Cheng H, et al. The anti-parasitic drug suramin potently inhibits formation of seminal amyloid fibrils and their interaction with HIV-1[J]. Journal of Biological Chemistry. 2019: jbc. RA118. 006797. 10. Zhang R, Zhang F, Sun Z, et al. LINE-1 Retrotransposition Promotes the Development and Progression of Lung Squamous Cell Carcinoma by Disrupting the Tumor Suppressor Gene FGGY[J]. Cancer research. 2019: canres. 0076.2019. |
| Citations | 1. Zhang R, Zhang F, Sun Z, et al. LINE-1 Retrotransposition Promotes the Development and Progression of Lung Squamous Cell Carcinoma by Disrupting the Tumor Suppressor Gene FGGY. Cancer Research. 2019: canres. 0076 2. Tan S, Li J Q, Cheng H, et al. The anti-parasitic drug suramin potently inhibits formation of seminal amyloid fibrils and their interaction with HIV-1. Journal of Biological Chemistry. 2019: jbc. RA118. 006797 3. Tan S, Li W, Li Z, et al. A Novel CXCR4 Targeting Protein SDF-1/54 as an HIV-1 Entry Inhibitor. Viruses. 2019, 11(9): 874 4. Wu Y, Yang J, Duan C, et al. Simultaneous determination of antiretroviral drugs in human hair with liquid chromatography-electrospray ionization-tandem mass spectrometry. Journal of Chromatography B. 2018 Apr 15;1083:209-221 |