IOWH032

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IOWH032

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	1191252-49-9
规格:	≥98%

包装与价格：

包装	价格(元)
5mg	询价
10mg	询价
25mg	询价
50mg	询价
100mg	询价
500mg	询价
1g	询价

IOWH-032 (IOWH032; IOWH 032) is a potent and synthetic CFTR (Cystic fibrosis transmembrane conductance regulator) inhibitor with antifibrotic activity. It inhibits CFTR with IC50s of 1.01 μM and in CHO-CFTR and T84-CFTR cell based assays, respectively. IOWH-032 rapidly blocked and potentiated hCFTR activity in a concentration-dependent manner with apparent Kd value of 6.1 nM and 0.64 nM, respectively. However, IOWH-032 did not potentiate and only blocked mCFTR with an apparent Kd value of 42.9 μM.

理化性质和储存条件

Molecular Weight (MW)	545.18
Formula	C22H15Br2N3O4
CAS No.	1191252-49-9
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 100 mg/mL (183.4 mM)
	Water: <1 mg/mL
	Ethanol: <1 mg/mL
Other info	Chemical Name: 3-(3,5-dibromo-4-hydroxyphenyl)-N-(4-phenoxybenzyl)-1,2,4-oxadiazole-5-carboxamide . InChi Key: DSFNLJXHXBIKDS-UHFFFAOYSA-N InChi Code: InChI=1S/C22H15Br2N3O4/c23-17-10-14(11-18(24)19(17)28)20-26-22(31-27-20)21(29)25-12-13-6-8-16(9-7-13)30-15-4-2-1-3-5-15/h1-11,28H,12H2,(H,25,29) SMILES Code: O=C(C1=NC(C2=CC(Br)=C(O)C(Br)=C2)=NO1)NCC3=CC=C(OC4=CC=CC=C4)C=C3
Synonyms	IOWH032; IOWH-032; IOWH 032

实验参考方法

In Vitro	In vitro activity: IOWH032 shows inhibitory activity against CFTR in T84-CFTR cell based assays with IC50 of 6.87 μM.
In Vivo	In a mouse closed-loop model, IOWH032 causes a statistical significant inhibition against cholera toxin (CTX) induced secretion. IOWH032 (5 mg/kg) reduces the fecal output index by ~70% in a cecetomized rat model.
Animal model	A cecetomized rat model
Formulation & Dosage	Dissolved in DMSO; ~5 mg/kg; p.o.
References	Future Med Chem. 2011;3(10):1317-25.