ASP7663

Research use only, not for human use.

ASP7663 is a?TRPA1 Receptor Agonist?and exhibiting an abdominal analgesic effect in vivo.?

ASP7663 is a?TRPA1 Receptor Agonist?and exhibiting an abdominal analgesic effect in vivo.?

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) 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.

ASP7663 significantly improves the loperamide-induced delay in colonic transit in mice. ASP7663 (orally, 0.3 and 1 mg/kg) significantly shortens the prolonged bead expulsion time caused by loperamide.ASP7663 (orally, 1 and 3 mg/kg) exhibits inhibitory effects on colorectal distension in rat. 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.

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Membrane Transporter/Ion Channel

TRP/TRPV Channel

TRPA1

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1190217-35-6

263.26

C14H14FNO3?

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (189.93 mM)

CC(C)CN1C(=O)\C(=C\C(O)=O)c2cccc(F)c12

(2E)-2-[7-Fluoro-12-dihydro-1-(2-methylpropyl)-2-oxo-3H-indol-3-ylidene]acetic acid

(-20℃)

With Ice Pack

≥ 2 years