Nevirapine (NSC 641530)

製品コードS1742 バッチS174201

印刷

化学情報

 Chemical Structure Synonyms NSC 641530,NVP Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C15H14N4O

分子量 266.3 CAS No. 129618-40-2
Solubility (25°C)* 体外 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.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Nevirapine (NSC 641530,NVP) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used to treat HIV-1 infection and AIDS.
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]

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]

プロトコル(参考用のみ)

カスタマーフィードバック

Data from [Data independently produced by , , Sci Transl Med, 2014, 6(262): 262ra157 ]

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。