A TRPA1 agonist; induces calcium influx in HEK293 cells expressing human

ASP7663 – 5 mg

Brand:
Cayman
CAS:
1190217-35-6
Storage:
-20
UN-No:
Non-Hazardous - /

ASP7663 is a transient receptor potential ankyrin 1 (TRPA1) agonist.{61076} 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 (Item No. 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 (Item No. 11923). ASP7663 (0.3 mg/kg, p.o.) reduces the number of abdominal contractions induced by colorectal distension in mice.  

 

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Description

A TRPA1 agonist; induces calcium influx in HEK293 cells expressing human, rat, or mouse TRPA1 (EC50s = 0.51, 0.54, and 0.5 µM, respectively) and stimulates 5-HT release from QGP-1 enterochromaffin cells that endogenously express TRPA1 (EC50 = 72.5 µM); reduces colonic transit time in clonidine- or loperamide-induced mouse models of constipation at 1 mg/kg; reduces the number of abdominal contractions induced by colorectal distension in mice at 0.3 mg/kg

Formal name: (2E)-2-[7-fluoro-1,2-dihydro-1-(2-methylpropyl)-2-oxo-3H-indol-3-ylidene]-acetic acid

Synonyms: 

Molecular weight: 263.3

CAS: 1190217-35-6

Purity: ≥95%

Formulation: A crystalline solid

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