Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
説明 | 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. |
ターゲット&IC50 | EP1 receptor (human):1410 nM(ki), EP4 receptor (human):(EC50)17 nM, EP4 receptor (human):(ki)2.57 nM, EP3 receptor (human):160 nM(EC50), EP3 receptor (human):32.4 nM(ki), EP2 receptor (human):1000 nM(EC50), EP2 receptor (human):1540 nM(ki), IP receptor (human):52.9 nM(ki) |
In vitro | 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]. |
分子量 | 460.52 |
分子式 | C24H30F2N4O3 |
CAS No. | 1215192-68-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. 詳細
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KAG-308 1215192-68-9 GPCR/G Protein Immunology/Inflammation Prostaglandin Receptor KAG308 KAG 308 Inhibitor inhibitor inhibit