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1190217-35-6

中文名稱 ASP 7663;ASP-7663;ASP7663
英文名稱 ASP7663
CAS 1190217-35-6
分子式 C14H14FNO3
分子量 263.26
MOL 文件 1190217-35-6.mol
更新日期 2023/03/20 15:41:27
1190217-35-6 結(jié)構(gòu)式 1190217-35-6 結(jié)構(gòu)式

基本信息

中文別名
化合物ASP7663
英文別名
ASP7663
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)

儲存條件-20°C儲存
溶解度DMSO: 25 mg/ml,Ethanol: 25 mg/ml
形態(tài)結(jié)晶固體
顏色Light yellow to orange

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335

常見問題列表

生物活性
ASP7663 是具有口服活性的、選擇性的 TRPA1 激動劑。ASP7663 具有抗便秘和抗腹痛的活性。
體外研究

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.

體內(nèi)研究

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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