Nevirapine | 奈韦拉平 | MedChemExpress (MCE)

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Nevirapine

CAS No. : 129618-40-2

MCE 国际站：Nevirapine

产品活性：Nevirapine (BI-RG 587) 是用于研究 HIV/AIDS 的 HIV-1 逆转录酶非核苷抑制剂，K_i 值为 270 μM。

研究领域：Anti-infection

作用靶点：HIV  |  Reverse Transcriptase  |  Parasite

In Vitro: Nevirapine itself is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (K_i=270 μM). Nevirapine has been used as a re-differentiation agent to treat cancers in several human cancer models. At all doses (100, 200, 350, 500 μM) tested, nevirapine significantly inhibits cell proliferation after 48 h treatment. At high dose (500 μM), nevirapine significantly increases the percentage of apoptotic cells compared with control. Nevirapine is a potent and selective inhibitor (IC₅₀=10-100 nM) of the replication of a wide variety of HIV-1 strains in several cellular assays.

In Vivo: Nevirapine is available for use in combination with nucleoside HIV-1 reverse transcriptase inhibitors (e.g., zidovudine, didanosine, etc.). Nevirapine has received FDA approval for use in combination with HIV-1 protease inhibitors (e.g., saquinavir, ritonavir, indinavir, etc.). In humans, nevirapine is eliminated primarily in the urine as glucuronide conjugates of 2-, 3-, 8-, and 12-hydroxynevirapine. Nevirapine is completely absorbed in both sexes of mouse, rat, rabbit, monkey, and chimpanzee. Nevirapine is extensively metabolized in both sexes of all animal species studied. Nevirapine (9 mg/kg, 18 mg/kg and 36 mg/kg) shows significant reduction in ulcer severity score and ulcer index as compared to the control

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