Atazanavir

製品コードS4662 バッチS466203

印刷

化学情報

Chemical Structure 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.
* <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 (Latazanavir, Zrivada, Reyataz, BMS-232632) is an azapeptide and HIV-protease inhibitor that is used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents. Atazanavir is a substrate and inhibitor of cytochrome P450 isozyme 3A (CYP3A4) and an inhibitor and inducer of P-glycoprotein.
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[1]. 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[3].
in vivo Atazanavir has excellent oral bioavailability in the range of 60-70%[1].

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。

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