产品描述
KAG-308 is an effective selective and orally active agonist of the EP4 receptor (Ki: 2.57 nM and EC50: 17 nM for human EP4 receptor), more selective over EP1, EP2, EP3, and IP receptor. KAG-308 suppresses colitis and promotes histological mucosal healing, which potently inhibits TNF-α production.
体外活性
KAG-308 shows effective agonist activity for human and mouse EP4 (EC50: 0.15 nM and 1.0 nM, respectively in the dual luciferase reporter assay). KAG-308 shows a Ki and EC50 values of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over human EP1 (Ki, 1410 nM; EC50, 1000 nM), EP2 (Ki, 1540 nM; EC50, 1000 nM), EP3 (Ki, 32.4 nM; EC50, 160 nM) and IP receptor (Ki, 52.9 nM; EC50, >10000 nM) [1].
Cas No.
1215192-68-9
分子式
C24H30F2N4O3
分子量
460.52
别名
KAG-308
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years