Cas No.: | 244101-03-9 |
Synonyms: | L-826,266 |
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 |
Formula: | C27H21BrClNO4S |
M.Wt: | 570.9 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | 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). |