| Bioactivity | 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]. | ||||||||||||
| Target | EC50: 79 nM (F508del CFTR) and 497 nM (G551D CFTR) | ||||||||||||
| Invitro | 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 Vivo | 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]. | ||||||||||||
| Name | Icenticaftor | ||||||||||||
| CAS | 1334546-77-8 | ||||||||||||
| Formula | C12H13F6N3O3 | ||||||||||||
| Molar Mass | 361.24 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [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. |
Icenticaftor
CAS: 1334546-77-8 F: C12H13F6N3O3 W: 361.24
Icenticaftor (QBW251) is an orally active CFTR channel potentiator, with EC50s of 79 nM and 497 nM for F508del and G551D
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