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IOWH032

Names

[ CAS No. ]:
1191252-49-9

[ Name ]:
IOWH032

[Synonym ]:
unii-8y3gdt6ywv
1,2,4-Oxadiazole-5-carboxamide, 3-(3,5-dibromo-4-hydroxyphenyl)-N-[(4-phenoxyphenyl)methyl]-
s7329
3-(3,5-Dibromo-4-hydroxyphenyl)-N-(4-phenoxybenzyl)-1,2,4-oxadiazole-5-carboxamide
IOWH032
IOWH-032
iowh 032

Biological Activity

[Description]:

IOWH-032 is a novel and potent CFTR inhibitor (IC50=1.01 uM) in T84 and CHO-CFTR cell based assays.IC50 value: 1.01 uM (CHO-CFTR FLIPR) [1]Target: CFTRProfiling of iOWH032 showed it to be a CFTR inhibitor in T84 and CHO-CFTR cell based assays. It also demonstrated statistical significant inhibition at both 100 g & 10 g doses in the mouse closed-loop model. iOWH032 was further profiled in a cecetomized rat model. iOWH032 reduced the fecal output index by ~70%, compared to vehicle (choleratoxin), up to 8 hours after a single 5 mg/kg po dose.

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> CFTR
Research Areas >> Metabolic Disease

[References]

[1]. Doyle K, et al. Inhibitors Of The CFTR Chloride Ion Channel As Potential Treatment For Acute Secretory Diarrhea: Development Of 5-membered Heterocycles Suitable For Pre-clinical Evaluation

[2]. de Hostos EL, et al. Developing novel antisecretory drugs to treat infectious diarrhea. Future Med Chem. 2011 Aug;3(10):1317-25.


[Related Small Molecules]

Lumacaftor (VX-809) | CFTR(inh)-172 | Tezacaftor(VX-661) | GlyH 101 | GLPG1837 | PPQ 102 | BPO-27 racemate | KM 11060

Chemical & Physical Properties

[ Density]:
1.7±0.1 g/cm3

[ Molecular Formula ]:
C22H15Br2N3O4

[ Molecular Weight ]:
545.180

[ Exact Mass ]:
542.942932

[ PSA ]:
97.22000

[ LogP ]:
7.13

[ Index of Refraction ]:
1.665

[ Storage condition ]:
-20°C

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds