L-902,688 是一种有效、选择性和口服活性的 EP4 受体激动剂,Ki 为 0.38 nM,EC50 为 0.6 nM。
Cas No. | 634193-54-7 |
Canonical SMILES | [H]N1C(CCCCCCN2[C@@H](/C=C/[C@](O)([H])C(F)(F)C3=CC=CC=C3)CCC2=O)=NN=N1 |
分子式 | C21H27F2N5O2 |
分子量 | 419.5 |
溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | Prostaglandin E2 (PGE2) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption, cancer, and atherosclerosis. L-902,688 is a highly potent agonist of the human PGE2 receptor, EP4. It demonstrates a Ki value of 0.38 nM and an EC50 value of 0.6 nM and is >4,000-fold selective for EP4 over other EP and prostanoid receptors. L-902,688 induces thermal hyperalgesia when injected into guinea pig forepaw and increases vasodilation of human pulmonary vein. |