Nevirapine (NSC 641530)

製品コードS1742 バッチS174202

印刷

化学情報

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 1 40%PEG300 2 5%Tween80 3 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 1 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) は、HIV-1感染症とAIDSの治療に使用される非ヌクレオシド Reverse Transcriptase 阻害剤 (NNRTI) です。
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 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. 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. It is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki = 270 mM). 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.
in vivo	Nevirapine (NSC 641530) is metabolized to 4-CANVP as a major metabolite in all male animals and in female mice, dogs, and monkeys. 3-OHNVP is a major fecal metabolite in all animals except for the male rat. In the bile of rats, 4-CANVP is a major metabolite along with 12-OHNVP glucuronide.

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/

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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：

LINE-1 activation in the cerebellum drives ataxia [ Neuron, October 19, 2022, 3278-3287.e8]	PubMed: 36070749
In vitro comparison of the susceptibilities of the same drug resistance mutations to reverse-transcriptase inhibitors of subtype B and CRF01_AE HIV-1 strains [ Scientific Reports, October 15, 2025, 15(1)]	PubMed: 41093949
Bcl-2 Antagonist Obatoclax Reactivates Latent HIV-1 via the NF-κB Pathway and Induces Latent Reservoir Cell Apoptosis in Latently Infected Cells [ ACS Infectious Diseases, November 10, 2023, 2105-2118]	PubMed: 37796279
PARP1 depletion induces RIG-I-dependent signaling in human cancer cells [ PLoS One, March 28, 2018, e0194611]	PubMed: 29590171
Discovery of Benzisothiazolone Derivatives as Bifunctional Inhibitors of HIV-1 Reverse Transcriptase DNA Polymerase and Ribonuclease H Activities [ Biomolecules, July 9, 2024, 819]	PubMed: 39062532
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

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。