Daclatasvir Dihydrochloride

製品コードS5062 バッチS506201

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C40H50N8O6.2HCl
分子量 811.8 CAS No. 1009119-65-6
Solubility (25°C)* 体外 DMSO 100 mg/mL (123.18 mM)
Water 100 mg/mL (123.18 mM)
Ethanol 100 mg/mL (123.18 mM)
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。

 5mg/ml (6.16mM) Taking the 1 mL working solution as an example, add 50 μL of 100 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。

 0.71mg/ml (0.87mM) Taking the 1 mL working solution as an example, add 50 μL of 14.2 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 Daclatasvirは、慢性HCVジェノタイプ1および3型感染症の治療に用いられる、C型肝炎ウイルス（HCV）のNS5A領域を阻害する経口抗ウイルス薬です。
in vitro Daclatasvir exhibited potent inhibition in all of the wild-type replicons and hybrid replicons representing the range of genotypes and subtypes. daclatasvir induces an alteration in the subcellular localization of NS5A, which inhibits the formation and activation of HCV RCs. Daclatasvir was found to have a high potency across all HCV genotypes with half-maximum effective concentrations (EC50) ranging from 9 to 146 pM. While it is pangenotypic, it has a low barrier to resistance against the subtype of Genotype 1a.
in vivo Daclatasvir has good bioavailability in rats, dogs and cynomolgus monkey (F%= 50, 108 and 38 respectively).

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/22962522/
  • https://pubmed.ncbi.nlm.nih.gov/23931586/

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：

Combination of antiviral drugs inhibits SARS-CoV-2 polymerase and exonuclease and demonstrates COVID-19 therapeutic potential in viral cell culture [ Commun Biol, 2022, 5(1):154] PubMed: 35194144
In vitro antiviral activity of the anti-HCV drugs daclatasvir and sofosbuvir against SARS-CoV-2, the aetiological agent of COVID-19 [ J Antimicrob Chemother, 2021, 76(7):1874-1885] PubMed: 33880524
Correlation of hepatitis C virus-mediated endoplasmic reticulum stress with autophagic flux impairment and hepatocarcinogenesis [ Med Mol Morphol, 2021, 10.1007/s00795-020-00271-5] PubMed: 33386512
Combination of Antiviral Drugs to Inhibit SARS-CoV-2 Polymerase and Exonuclease as Potential COVID-19 Therapeutics [ bioRxiv, 2021, 2021.07.21.453274] PubMed: 34312622
Fluoxazolevir inhibits hepatitis C virus infection in humanized chimeric mice by blocking viral membrane fusion [ Nat Microbiol, 2020, 10.1038/s41564-020-0781-2] PubMed: 32868923
Sofosbuvir Activates EGFR-Dependent Pathways in Hepatoma Cells with Implications for Liver-Related Pathological Processes. [ Cells, 2020, 17;9(4) pii: E1003] PubMed: 32316635
Sofosbuvir Activates EGFR-Dependent Pathways in Hepatoma Cells with Implications for Liver-Related Pathological Processes [ Cells, 2020, 9(4)E1003] PubMed: 32316635
Differential modulation of hepatitis C virus replication and innate immune pathways by synthetic calcitriol-analogs [ J Steroid Biochem Mol Biol, 2018, 183:142-151] PubMed: 29885880

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。