| 产品描述: | 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。 |
| 靶点: |
EC50: 79 nM (F508del CFTR) and 497 nM (G551D CFTR);CFTR |
| 体外研究: |
Icenticaftor (QBW251), an orally bioavailable small molecule CFTR potentiator, can restore CFTR function in specific CFTR genotypes as well as wild-type CFTR. |
| 体内研究: |
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. |
| 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. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.768 ml |
13.841 ml |
27.682 ml |
| 5 mM |
0.554 ml |
2.768 ml |
5.536 ml |
| 10 mM |
0.277 ml |
1.384 ml |
2.768 ml |
| 50 mM |
0.055 ml |
0.277 ml |
0.554 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |