产品说明书

Icenticaftor

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Chemical Structure| 1334546-77-8 同义名 : QBW251;NVP-QBW251
CAS号 : 1334546-77-8
货号 : A1277845
分子式 : C12H13F6N3O3
纯度 : 98%
分子量 : 361.24
MDL号 : MFCD31631074
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 145 mg/mL(401.39 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Icenticaftor, also known as QBW251, is an orally active CFTR channel potentiator with EC50 values of 79 nM and 497 nM for F508del CFTR and G551D CFTR, respectively.Icenticaftor is used in chronic obstructive pulmonary disease (COPD) and cystic fibrosis studies[1].Icenticaftor is an orally bioactive small molecule CFTR potentiator that restores the function of specific mutant and wild-type CFTRs[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.77mL

0.55mL

0.28mL

13.84mL

2.77mL

1.38mL

27.68mL

5.54mL

2.77mL
参考文献

[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.