Asunaprevir

製品コードS4935 バッチS493502

印刷

化学情報

Synonyms

BMS-650032

Storage
(From the date of receipt)

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

化学式

C₃₅H₄₆ClN₅O₉S

分子量

748.29

CAS No.

630420-16-5

Solubility (25°C)*

体外

DMSO

100 mg/mL (133.63 mM)

Ethanol

100 mg/mL (133.63 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

	5% DMSO 1 95% Corn oil	13.0mg/ml
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/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	Asunaprevir is an orally bioavailable inhibitor of the hepatitis C virus enzyme serine protease NS3 that is necessary for protein processing required for viral replication.
in vitro	Asunaprevir (ASV) competitively binds to the NS3/4A protease complex, with Ki values of 0.4 and 0.24 nM against recombinant enzymes representing genotypes 1a (H77) and 1b (J4L6S), respectively. Asunaprevir is high selective without any significant activity against the closely related GB virus-B NS3 protease and a panel of human serine or cysteine proteases. In cell culture, ASV inhibits replication of HCV replicons representing genotypes 1 and 4, with 50% effective concentrations (EC50s) ranging from 1 to 4 nM, and has weaker activity against genotypes 2 and 3 (EC50, 67-1162 nM). Selectivity is again demonstrated by the absence of activity (EC50, >12 μM) against a panel of other RNA viruses^[1].
in vivo	Plasma and tissue exposures in vivo in several animal species indicate that ASV displays a hepatotropic disposition (liver-to-plasma ratios ranging from 40- to 359-fold across species). Twenty-four hours postdose, liver exposures across all species tested are ≥110-fold above the inhibitor EC50s observed with HCV genotype-1 replicons^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Huh 7.5.1 cells
	濃度	1 or 10 nM
	反応時間	3, 6, 24, and 48 h
	実験の流れ	--
動物実験	動物モデル	male FVB mice, Sprague-Dawley rats, male beagles, male cynomolgus monkeys
	投薬量	5 mg/kg (mice); 3, 5, 10, and 15 mg/kg (rats); 3 or 6 mg/kg (Dogs); 3 mg/kg (Monkeys)
	投与方法	by oral gavage

参考

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：

METTL3-Dependent N6-Methyladenosine Modification Programs Human Neural Progenitor Cell Proliferation [ Int J Mol Sci, 2023, 10.3390/ijms242115535]	PubMed: 37958523
Genetic instability from a single S phase after whole-genome duplication [ Nature, 2022, 604(7904):146-151]	PubMed: 35355016
Going Viral: An Investigation into the Chameleonic Behaviour of Antiviral Compounds [ Chemistry, 2022, e202202798.]	PubMed: 36286339
Hepatitis C virus drugs that inhibit SARS-CoV-2 papain-like protease synergize with remdesivir to suppress viral replication in cell culture [ Cell Rep, 2021, 35(7):109133]	PubMed: 33984267
Development of a Cell-Based Luciferase Complementation Assay for Identification of SARS-CoV-2 3CLpro Inhibitors [ Viruses, 2021, 13(2)173]	PubMed: 33498923
Mechanisms of genetic instability in a single S-phase following whole genome doubling [ bioRxiv, 2021, 10.1101/2021.07.16.452672]	PubMed: None

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。