1190217-35-6
基本信息
ASP7663 >=98% (HPLC)
ASP 7663
ASP-7663
ASP7663
(2E)-2-[7-Fluoro-1,2-dihydro-1-(2-methylpropyl)-2-oxo-3H-indol-3-ylidene]acetic acid
Acetic acid, 2-[7-fluoro-1,2-dihydro-1-(2-methylpropyl)-2-oxo-3H-indol-3-ylidene]-, (2E)-
物理化學(xué)性質(zhì)
常見問題列表
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.
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. |