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CAS No.: 1191252-49-9

IOWH-032 Catalog No. CSN13745

Synonyms: IOWH-032

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

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靶点选择性

生物活性

实验方案

技术信息

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].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01823939	Diarrhea Chol... more >>era Collapse <<	Phase 1	Completed	-	Bangladesh ... more >> Dhaka Hospital - icddr,b (International Centre for Diarrhoeal Disease Research, Bangladesh) Mohakhali, Dhaka, Bangladesh, 1212 Collapse <<
NCT02111304	Secretory Diarrhea	Phase 2	Withdrawn(Trial was never init... more >>iated due to PATH executive decision.) Collapse <<	May 2016	Bangladesh ... more >> International Centre for Diarrhoeal Disease Research, Bangladesh Dhaka, Bangladesh, 1212 Collapse <<

参考文献

[1] Cui G, Khazanov N, Stauffer BB, et al. Potentiators exert distinct effects on human, murine, and Xenopus CFTR. Am J Physiol Lung Cell Mol Physiol. 2016 Aug 1;311(2):L192-207.
[2] de Hostos EL, Choy RK, Nguyen T. Developing novel antisecretory drugs to treat infectious diarrhea. Future Med Chem. 2011 Aug;3(10):1317-25.
[3] de Hostos EL, Choy RK, Nguyen T. Developing novel antisecretory drugs to treat infectious diarrhea. Future Med Chem. 2011 Aug;3(10):1317-25
[4] Cui G, Khazanov N, Stauffer BB, et al. Potentiators exert distinct effects on human, murine, and Xenopus CFTR. Am J Physiol Lung Cell Mol Physiol. 2016 Aug 1;311(2):L192-207

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8343 mL
- 9.1713 mL
- 18.3426 mL
- 5 mM
- 0.3669 mL
- 1.8343 mL
- 3.6685 mL
- 10 mM
- 0.1834 mL
- 0.9171 mL
- 1.8343 mL

技术信息

CAS号

1191252-49-9

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H15Br2N3O4

运输

蓝冰

分子量

545.18

别名

IOWH-032

溶解度

DMSO	100.0 mg/mL (183.4 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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