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IOWH-032

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Chemical Structure| 1191252-49-9 同义名 : -
CAS号 : 1191252-49-9
货号 : A170946
分子式 : C22H15Br2N3O4
纯度 : 99%+
分子量 : 545.18
MDL号 : MFCD25977119
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(192.6 mM)，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
靶点

  • CFTR

    CFTR, IC50:1.01 μM
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 Kd of 6.1 nM. Through time, it also potentiated hCFTR in a concentration-dependent manner with an apparent Kd 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.83mL

0.37mL

0.18mL

9.17mL

1.83mL

0.92mL

18.34mL

3.67mL

1.83mL
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