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Icenticaftor
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Icenticaftor图片
CAS NO:1334546-77-8
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
Icenticaftor (QBW251) 是一种具有口服活性 CFTR 通道增强剂,F508del 和 G551D CFTR 的 EC50 分别为 79 nM 和 497 nM。Icenticaftor 可用于慢性阻塞性肺疾病 (COPD) 和囊性纤维化研究。
Cas No.1334546-77-8
别名3-氨基-6-甲氧基-N-[(2S)-3,3,3-三氟-2-羟基-2-甲基丙基]-5-(三氟甲基)-2-吡啶甲酰胺,QBW251
分子式C12H13F6N3O3
分子量361.24
溶解度DMSO : 150 mg/mL (415.24 mM; ultrasonic and warming and heat to 60°C)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Icenticaftor (QBW251) is an orally active CFTR channel potentiator, with EC50s of 79 nM and 497 nM for F508del and G551D CFTR, respectively. Icenticaftor can be used for chronic obstructive pulmonary disease (COPD) and cystic fibrosis research[1].

Icenticaftor (QBW251), an orally bioavailable small molecule CFTR potentiator, can restore CFTR function in specific CFTR genotypes as well as wild-type CFTR[2].

In Sprague-Dawley rats, the pharmacokinetic profile of Icenticaftor is established. After oral administration at a dose of 3 mg/kg, the oral bioavailability is 90%, and AUClast is 20?635 nmol/L•h[1].

[1]. Darren Le Grand, et al. Discovery of Icenticaftor (QBW251), a Cystic Fibrosis Transmembrane Conductance Regulator Potentiator with Clinical Efficacy in Cystic Fibrosis and Chronic Obstructive Pulmonary Disease. J Med Chem. 2021 Jun 10;64(11):7241-7260.
[2]. Steven M Rowe, et al. Efficacy and Safety of the CFTR Potentiator Icenticaftor (QBW251) in COPD: Results from a Phase 2 Randomized Trial. Int J Chron Obstruct Pulmon Dis. 2020 Oct 5;15:2399-2409.