ASP 7663;ASP-7663;ASP7663

ASP 7663;ASP-7663;ASP7663

中文名称ASP 7663;ASP-7663;ASP7663
中文同义词化合物ASP7663;ASP 7663,TRPA1激活剂
英文名称ASP7663
英文同义词ASP7663;(2E)-2-[7-Fluoro-1,2-dihydro-1-(2-methylpropyl)-2-oxo-3H-indol-3-ylidene]acetic acid;ASP 7663;ASP-7663;ASP7663;Acetic acid, 2-[7-fluoro-1,2-dihydro-1-(2-methylpropyl)-2-oxo-3H-indol-3-ylidene]-, (2E)-;ASP7663 >=98% (HPLC);pain,ASP-7663,inhibit,TRP Channel,ASP7663,Transient receptor potential channels,Inhibitor,ASP 7663
CAS号1190217-35-6
分子式C14H14FNO3
分子量263.26
EINECS号
相关类别
Mol文件1190217-35-6.mol
结构式ASP 7663;ASP-7663;ASP7663 结构式

ASP 7663;ASP-7663;ASP7663 性质

储存条件Store at -20°C
溶解度DMSO:25mg/mL,乙醇:25mg/mL
形态结晶固体
颜色浅黄至橙色

ASP 7663;ASP-7663;ASP7663 用途与合成方法

ASP7663 是具有口服活性的、选择性的 TRPA1 激动剂。ASP7663 具有抗便秘和抗腹痛的活性。

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.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/04/30HY-101907ASP76631 mg419元
2024/04/30HY-101907ASP 7663;ASP-7663;ASP7663
ASP7663
1190217-35-65mg1000元

ASP 7663;ASP-7663;ASP7663 上下游产品信息

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