CAS:1191252-49-9IOWH-032

IOWH-032 is a potent CFTR inhibitor (IC50=1.01 μM) in T84 and CHO-CFTR cell based assays.

规格	价格	促销价格	库存

18817579266

立即询价

咨询

18817579266

立即询价

实验数据

技术信息

CAS号

1191252-49-9

储存条件

分子式

C22H15Br2N3O4

运输

蓝冰

分子量

545.18

别名

溶解度

动物实验配方

生物活性

靶点 CFTR

IC50:1.01μM
描述The cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel, belonging to the ABC family of transporters, lies at the heart of hypersecretion associated with AWD (acute watery diarrhea) caused by enterotoxigenic bacteria. IOWH032, chloride channel blocker, is a synthetic CFTR inhibitor with antisecretory activity developed by OneWorld Health and currently in Phase I clinical trials to treat diarrhea^[3]. During a ~50s extracellular exposure to 5 nM IOWH-032, hCFTR was blocked. Specificly, IOWH-032 blocked hCFTR rapidly in a concentration-dependent manner with apparent K_d of 6.1 nM. Through time, it also potentiated hCFTR in a concentration-dependent manner with an apparent K_d of 0.64 nM. Moreover, 20 nM IOWH-032 potentiated F508del-hCFTR expressed in Xenopus oocytes^[4]. In two animal models of secretory diarrhea, injection of iOWH032 directly into intestinal loops inhibited secretion by nearly 70% as measured on a semi-quantitative fecal output scale^[3].