Icenticaftor |
| Catalog No.GC63353 |
Icenticaftor(QBW251)는 F508del 및 G551D CFTR에 대해 각각 79nM 및 497nM의 EC50을 갖는 경구 활성 CFTR 채널 강화제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1334546-77-8
Sample solution is provided at 25 µL, 10mM.
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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.
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)
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