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Formula | C15H14N4O |
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Molecular Weight | 266.3 | CAS No. | 129618-40-2 | |
Solubility (25°C)* | In vitro | DMSO | 53 mg/mL (199.02 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Nevirapine (NSC 641530,NVP) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used to treat HIV-1 infection and AIDS. | |
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In vitro | Nevirapine (NVP) itself is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki = 270 mM). [1] 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. [2] 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. [3] 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. [4] |
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In vivo | 4-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. [5] |
Data from [Data independently produced by , , Sci Transl Med, 2014, 6(262): 262ra157 ]
Biological and Structural Analyses of New Potent Allosteric Inhibitors of HIV-1 Integrase [ Antimicrob Agents Chemother, 2023, 67(7):e0046223] | PubMed: 37310224 |
DNA ultra-sensitive quantification, a technology for studying HIV unintegrated linear DNA [ Cell Rep Methods, 2023, 3(4):100443] | PubMed: 37159665 |
Reduction of CD8 T cell functionality but not inhibitory capacity by integrase inhibitors [ J Virol, 2022, JVI0173021] | PubMed: 35019724 |
Unexpected similarity between HIV-1 reverse transcriptase and tumor necrosis factor binding sites revealed by computer vision [ J Cheminform, 2021, 13(1):90] | PubMed: 34814950 |
A synthetic resveratrol analog termed Q205 reactivates latent HIV-1 through activation of P-TEFb [ Biochem Pharmacol, 2021, 197:114901] | PubMed: 34971588 |
Limitations of dual-fluorescent HIV reporter viruses in a model of pre-activation latency. [ J Int AIDS Soc, 2019, 22(12):e25425] | PubMed: 31855322 |
Nonnucleoside Reverse Transcriptase Inhibitor Hypersusceptibility and Resistance by Mutation of Residue 181 in HIV-1 Reverse Transcriptase. [ Antimicrob Agents Chemother, 2019, 63(8)] | PubMed: 31160281 |
Antiretroviral potency of 4'-ethnyl-2'-fluoro-2'-deoxyadenosine, tenofovir alafenamide and second-generation NNRTIs across diverse HIV-1 subtypes. [ J Antimicrob Chemother, 2018, 73(10):2721-2728] | PubMed: 30053052 |
PARP1 depletion induces RIG-I-dependent signaling in human cancer cells [ PLoS One, 2018, 13(3):e0194611] | PubMed: 29590171 |
Semen enhances HIV infectivity and impairs the antiviral efficacy of microbicides. [Zirafi O, et al. Sci Transl Med, 2014, 6(262):262ra157] | PubMed: 25391483 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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