ASP7663

ASP7663 is a transient receptor potential ankyrin 1 (TRPA1) agonist. It induces calcium influx in HEK293 cells expressing human, rat, or mouse TRPA1 (EC50s = 0.51, 0.54, and 0.5 µM, respectively) and stimulates serotonin (5-HT) release from QGP-1 enterochromaffin cells that endogenously express TRPA1 (EC50 = 72.5 µM). It reduces colonic transit time in mouse models of constipation induced by clonidine (Cay-15949) or loperamide when administered orally at a dose of 1 mg/kg, an effect that can be blocked by vagotomy or the TRPA1 antagonist HC-030031 (Cay-11923). ASP7663 (0.3 mg/kg, p.o.) reduces the number of abdominal contractions induced by colorectal distension in mice.Formal Name: (2E)-2-[7-fluoro-1,2-dihydro-1-(2-methylpropyl)-2-oxo-3H-indol-3-ylidene]-acetic acid. CAS Number: 1190217-35-6. Molecular Formula: C14H14FNO3. Formula Weight: 263.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 25 mg/ml, Ethanol: 25 mg/ml. lambdamax: 224, 250, 255, 315 nm. SMILES: FC1=C2C(/C(C(N2CC(C)C)=O)=C\C(O)=O)=CC=C1. InChi Code: InChI=1S/C14H14FNO3/c1-8(2)7-16-13-9(4-3-5-11(13)15)10(14(16)19)6-12(17)18/h3-6,8H,7H2,1-2H3,(H,17,18)/b10-6+. InChi Key: RCVZUIGCNAAMIC-UXBLZVDNSA-N.