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    Nevirapine (BI-RG 587)
    Nevirapine (BI-RG 587)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1816
    CAS #: 129618-40-2Purity ≥98%

    Description: Nevirapine (also known as NSC 641530; BI-RG 587; NSC 641530; NVP) is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV-1 infection and AIDS. It inhibits HIV-1 reverse transcriptase with a Ki of 270 μM. As with other antiretroviral drugs, HIV rapidly develops resistance if nevirapine is used alone, so recommended therapy consists of combinations of three or more antiretrovirals. Nevirapine in triple combination therapy has been shown to suppress viral load effectively when used as initial antiretroviral therapy.  

    References: Drug Metab Dispos. 1999 Dec;27(12):1488-95; Drug Metab Dispos. 1999 Dec;27(12):1434-47.

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    Molecular Weight (MW)266.3
    CAS No.129618-40-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 53 mg/mL (199.0 mM)
    Water:<1 mg/mL
    Ethanol: <1 mg/mL
    Other infoChemical Name: 11-cyclopropyl-4-methyl-5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepin-6-one
    InChi Code: InChI=1S/C15H14N4O/c1-9-6-8-17-14-12(9)18-15(20)11-3-2-7-16-13(11)19(14)10-4-5-10/h2-3,6-8,10H,4-5H2,1H3,(H,18,20)
    SMILES Code: O=C1C2=CC=CN=C2N(C3CC3)C4=NC=CC(C)=C4N1
    SynonymsNSC 641530; BI-RG-587; BIRG 0587; BIRG587; HSDB 7164; Nevirapine; NSC 641530; NVP; trade name: Viramune; Viramune XR.

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    In Vitro

    In vitro activity: Nevirapine (NVP) itself is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki = 270 mM). Nevirapine is a non-nucleoside RT inhibitor with a well-characterized inhibitory activity on RT enzymes of retroviral origin. Nevirapine is also an effective inhibitor of the endogenous RT in murine and human cell lines. Nevirapine exposure rescues the differentiation block present in acute myeloid leukemia (AML) cell lines and primary blasts from two AML patients, as indicated by morphological, functional and immunophenotypic assays. Nevirapine, a dipyridodiazepinone, is a highly specific inhibitor of HIV-1 reverse transcriptase (RT) which exhibits an IC50 = 84 nM in enzyme assays and IC50 = 40nM against HIV-1 replication in cell culture. Nevirapine alters the cleavage specificity of the RNase H, resulting Nevirapine-induced stimulation of RNase H activity beyond the increase expected from the change in cleavage specificity.

    Kinase Assay: Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM.

    Cell Assay: 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.

    In Vivo4-CANVP is a major metabolite in all the male animals and the female mouse, dog, and monkey. 3-OHNVP is a major fecal metabolite in all animals except for the male rat. 4-CANVP is a major metabolite along with 12-OHNVP glucuronide in the bile of rats.
    Animal modelMice and rats
    Formulation & DosageRats: Nevirapine and [14C] Nevirapine are dissolved together in absolute ethanol and methylene chloride (1:1, v/v) with mild heating. The concentration of drug in suspension is 2 mg/mL (20 mg/kg, 26 μCi) for oral dosing to rats and 6.7 mg/mL (20.3 mg/kg, 10 μCi males, 8.9 μCi females) for intraduodenal administration to rats before bile collection. The i.v. dose is administered to rats (1.1 mg/kg, 20 μCi) as a solution in 20% ethanol/80% saline.
    Mice: Nevirapine and [14C] Nevirapine are dissolved together in absolute ethanol and methylene chloride (1:1, v/v) with mild heating. The concentration of drug in suspension is 2 mg/mL (20 mg/kg, 2.5 μCi) with a specific activity of 5.55 μCi/mg for oral dosing to mice.
    ReferencesDrug Metab Dispos. 1999 Dec;27(12):1488-95; Drug Metab Dispos. 1999 Dec;27(12):1434-47.

    These protocols are for reference only. InvivoChem does not independently validate these methods.


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