Nevirapine (NSC 641530)

製品コードS1742 バッチS174202

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
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 2.600mg/ml (9.76mM) Taking the 1 mL working solution as an example, add 50 μL of 52 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 0.660mg/ml (2.48mM) Taking the 1 mL working solution as an example, add 50 μL of 13.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <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 (NSC 641530) is a non-nucleoside RT inhibitor with a well-characterized inhibitory activity on RT enzymes of retroviral origin. It is also an effective inhibitor of the endogenous RT in murine and human cell lines. This compound itself is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki = 270 mM). [1] Its 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] As a dipyridodiazepinone, it 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] It alters the cleavage specificity of the RNase H, resulting in Nevirapine-induced stimulation of RNase H activity beyond the increase expected from the change in cleavage specificity. [4]
in vivo

Nevirapine (NSC 641530) is metabolized to 4-CANVP as a major metabolite in all male animals and in 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)

参考

  • https://pubmed.ncbi.nlm.nih.gov/10570031/
  • https://pubmed.ncbi.nlm.nih.gov/12747369/
  • https://pubmed.ncbi.nlm.nih.gov/1371691/
  • https://pubmed.ncbi.nlm.nih.gov/7533167/
  • https://pubmed.ncbi.nlm.nih.gov/10570025/

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：

Inhibiting EZH2 targets atypical teratoid rhabdoid tumor by triggering viral mimicry via both RNA and DNA sensing pathways [ Nat Commun, 2024, 15(1):9321] PubMed: 39472584
Discovery of Benzisothiazolone Derivatives as Bifunctional Inhibitors of HIV-1 Reverse Transcriptase DNA Polymerase and Ribonuclease H Activities [ Biomolecules, 2024, 14(7)819] PubMed: 39062532
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
LINE-1 activation in the cerebellum drives ataxia [ Neuron, 2022, 110(20):3278-3287.e8] PubMed: 36070749
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

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。