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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。
IOWH032图片
CAS NO:1191252-49-9
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
500mg电议
1g电议

产品介绍
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
FormulaC22H15Br2N3O4
CAS No.1191252-49-9
Storage-20℃ for 3 years in powder form
-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 VivoIn 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 modelA cecetomized rat model
Formulation & DosageDissolved in DMSO; ~5 mg/kg; p.o.
References

Future Med Chem. 2011;3(10):1317-25.