Atazanavir

製品コードS4662 バッチS466203

印刷

化学情報

Synonyms

Latazanavir, Zrivada, Reyataz, BMS-232632

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₃₈H₅₂N₆O₇

分子量

704.86

CAS No.

198904-31-3

Solubility (25°C)*

体外

DMSO

60 mg/mL (85.12 mM)

Ethanol

24 mg/mL (34.04 mM)

Water

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。	3mg/ml (4.26mM)	Taking the 1 mL working solution as an example, add 50 μL of 60 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。	0.43mg/ml (0.61mM)	Taking the 1 mL working solution as an example, add 50 μL of 8.6 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	Atazanavir（ラタザナビル、ザリバダ、レイアタッツ、BMS-232632）は、アザペプチドおよびHIVプロテアーゼ阻害剤であり、他の抗HIV薬と組み合わせてHIV感染症およびエイズの治療に使用されます。AtazanavirはチトクロームP450イソザイム3A（CYP3A4）の基質および阻害剤であり、P-glycoproteinの阻害剤および誘導剤です。
in vitro	Atazanavir has potent in vitro activity with 50 and 90% effective concentrations(EC50) of 2-5 nM and 9-15 nM respectively against wild type virus. This compound is able to potently induce endoplasmic reticulum (ER) stress response in malignant glioma cells, as indicated by elevated levels of GRP78 and CHOP, and activation of caspase-4, which leads to cell death.
in vivo	Atazanavir has excellent oral bioavailability in the range of 60-70%.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	The malignant glioma cell lines U251, LN229 and T98G
	濃度	0-100 μM
	反応時間	48 h
	実験の流れ	U251, T98G, and LN229 glioblastoma cell lines are exposed to increasing concentrations of nelfinavir and atazanavir. Cells cultured in 96-well plates are treated with drugs for 48 h, and cell growth and survival are determined by conventional MTT assay.
動物実験	動物モデル	The WT mice (FVB/NTac strain), TKO mice (FVB/N7 strain)
	投薬量	10 mg/kg
	投与方法	i.v.

参考

https://pubmed.ncbi.nlm.nih.gov/12225250/
https://pubmed.ncbi.nlm.nih.gov/24379203/
https://pubmed.ncbi.nlm.nih.gov/18006837/

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：

In Vitro Susceptibility of HIV Isolates with High Growth Capability to Antiretroviral Drugs [ Int J Mol Sci, 2022, 23(23)15380]	PubMed: 36499705
Going Viral: An Investigation into the Chameleonic Behaviour of Antiviral Compounds [ Chemistry, 2022, e202202798.]	PubMed: 36286339
HOPX Plays a Critical Role in Antiretroviral Drugs Induced Epigenetic Modification and Cardiac Hypertrophy [ Cells, 2021, 10(12)3458]	PubMed: 34943964
Characterization of fluorescent probe substrates to develop an efficient high-throughput assay for neonatal hepatic CYP3A7 inhibition screening [ Sci Rep, 2021, 11(1):19443]	PubMed: 34593846
Antiretroviral Drugs Regulate Epigenetic Modification of Cardiac Cells Through Modulation of H3K9 and H3K27 Acetylation [ Front Cardiovasc Med, 2021, 8:634774]	PubMed: 33898535
The neuropeptides VIP and PACAP inhibit SARS-CoV-2 replication in monocytes and lung epithelial cells, decrease production of proinflammatory cytokines, and VIP [ BioRxiv, 2021, 10.1101/2020.07.25.220806]	PubMed: None
Altered Gut Microbiome under Antiretroviral Therapy: Impact of Efavirenz and Zidovudine [ ACS Infect Dis, 2020, 10.1021/acsinfecdis.0c00536]	PubMed: 33346662
Discovery of M Protease inhibitors encoded by SARS-CoV-2 [ Antimicrob Agents Chemother, 2020, AAC.00872-20]	PubMed: 32669265
Calibrating the In Vitro-In Vivo Correlation for OATP-Mediated Drug-Drug Interactions with Rosuvastatin Using Static and PBPK Models [ Drug Metab Dispos, 2020, 48(12):1264-1270]	PubMed: 33037044
Selective cell death of latently HIV-infected CD4+ T cells mediated by autosis inducing nanopeptides. [ Cell Death Dis, 2019, 10(6):419]	PubMed: 31142734

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。