Nevirapine

SKU: orb1226598

Description

A potent and specific non-nucleoside inhibitor (NNRTI) of HIV-1 reverse transcriptase with Ki of 0.2 uM; shows no effect on feline and simian RT or any mammalian DNA polymerases; inhibits HIV-1 replication and protein p24 production.HIV Infection Approved(In Vitro):Nevirapine itself is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki=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.\n(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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 129618-40-2
• MW: 266.2979
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₄N₄O
• SMILES: O=C1C2=CC=CN=C2N(C3CC3)C4=NC=CC(C)=C4N1
• Target: HIV
• Solubility: 10 mM in DMSO

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BI-RG 587 | NSC 641530 | NVP

Quick Database Links

Gene Symbol

HIV