ASP7663

1190217-35-6

263.26

DMSO : 250 mg/mL (949.63 mM; Need ultrasonic)

Membrane Transporter/Ion Channel; Neuronal Signaling

ASP7663 is an orally active and selective TRPA1 agonist. ASP7663 exerts both anti-constipation and anti-abdominal pain actions^[1][2]. In Vitro: ASP7663 concentration dependently increases intracellular Ca²⁺ concentration in human, rat, and mouse TRPA1 expressed in HEK293 cells in a similar manner, with respective EC₅₀ 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) umol/L^[1].
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) umol/L^[1].
In Vivo: ASP7663 significantly improves the loperamide-induced delay in colonic transit in mice^[1].
ASP7663 (orally, 0.3 and 1 mg/kg) significantly shortens the prolonged bead expulsion time caused by loperamide^[1].
ASP7663 (orally, 1 and 3 mg/kg) exhibits inhibitory effects on colorectal distension in rat^[1].