Molecular Formula | C14H14FNO3 |
Molar Mass | 263.26 |
Solubility | DMSO: 25 mg/mL, clear |
Storage Condition | 2-8°C |
In vitro study | ASP7663 concentration dependently increases intracellular Ca 2+ concentration in human, rat, and mouse TRPA1 expressed in HEK293 cells in a similar manner, with respective EC 50 values (95% confidence interval [CI]) of 0.51 (0.40–0.66), 0.54 (0.41–0.72), and 0.50 (0.41–0.63) μmol/L. ASP7663 concentration-dependently stimulates 5-HT release from QGP-1 cells, a lineage of TRPA1-expressing EC cells, with an EC50 value of 72.5 (52.6–99.9) μmol/L. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.799 ml | 18.993 ml | 37.985 ml |
5 mM | 0.76 ml | 3.799 ml | 7.597 ml |
10 mM | 0.38 ml | 1.899 ml | 3.799 ml |
5 mM | 0.076 ml | 0.38 ml | 0.76 ml |
biological activity | ASP7663 is an orally active, selective TRPA1 agonist. ASP7663 has anti-constipation and anti-Abdominal Pain activity. |
Animal Model: | CRD model (colorectal distension in rat). |
Dosage: | 1 and 3 mg/kg. |
Administration: | Orally. |
Result: | Significantly reduced the number of abdominal contractions evoked during CRD at pressures of 30, 45, and 60 mmHg. ASP7663 also reduced the number of abdominal contractions by intravenous treatment. |