Nevirapine

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. (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.

129618-40-2

BI-RG 587 | NSC 641530 | NVP

Pharmacology & Drug Discovery

>98% (HPLC)

10 mM in DMSO

O=C1C2=CC=CN=C2N (C3CC3) C4=NC=CC (C) =C4N1

C15H14N4O

266.2979

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.