product name IOWH032
Description: IOWH032 is a synthetic CFTR inhibitor with IC50 of 1.01 μM in CHO-CFTR cell based assays. IOWH032 inhibited CFTR activity with IC50 value of 6.87 μM in T84-CFTR cell based assays [1]. 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.
References: Future Med Chem. 2011 Aug;3(10):1317-25.
545.18
Formula
C22H15Br2N3O4
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
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19406830
| In Vitro |
In vitro activity: IOWH032 shows inhibitory activity against CFTR in T84-CFTR cell based assays with IC50 of 6.87 μM. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
