L-826,266 是一种选择性和竞争性 EP3 受体拮抗剂。
| Cas No. | 244101-03-9 |
| Canonical SMILES | ClC(C=C1/C=C/C(NS(C2=C(OC)C=CC(Br)=C2)(=O)=O)=O)=CC=C1CC3=CC4=CC=CC=C4C=C3 |
| 分子式 | C27H21BrClNO4S |
| 分子量 | 570.9 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 10 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 | L-826,266 is a potent and selective competitive antagonist of the prostaglandin E2 receptor subtype EP3 (Ki = 0.8 nM). It also binds to the EP4 receptor (Ki = 715 nM) but does not bind to EP1 or EP2 receptors up to a concentration of 5,000 nM. L-826,266 inhibits vasoconstriction induced by the EP3 agonist sulprostone in a concentration-dependent manner (EC50s = 0.45-24.5 µM in isolated human pulmonary arteries). It also inhibits sulprostone-induced norepinephrine and serotonin release in rat cortex and norepinephrine release in rat vas deferens (pA2s = 7.56, 7.67, and 7.87, respectively). |
