L-826,266 is a potent and selective competitive antagonist of the prostaglandin E2 receptor subtype EP3 (Ki = 0.8 nM).
CAS:244101-03-9
分子式:C27H21BrClNO4S
分子量:570.9
纯度:98%
存储:Store at -20°C
Background:
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).