PF04418948是一种可口服的,选择性的前列腺素EP2受体拮抗剂,IC50为16 nM。
产品描述
PF-04418948 is a potent EP2 receptor antagonist (IC50 = 16 nM for human EP2 receptors). Displays over 2000-fold selectivity for EP2 receptors over EP1, EP3, EP4, DP1 amd CRTH2 receptors; exhibits<30% binding at a diverse panel of GPCRs and ion channels at a concentration of 10 μM. Inhibits PGE2-induced increases in intracellular cAMP; reverses PGE2-invoked relaxation of mouse trachea (IC50 = 2.7 nM).
体内活性
Eslicarbazepine acetate(ESL) has Anticonvulsant effects on the development of latrunculin A-induced seizures and paroxysmal EEG activity. ESL may also exhibit disease-modifying effects beyond suppressing just seizure activity, possibly by altering the development of a hyperexcitable network, as evidenced by the suppressed changes in glycine, taurine, glutamate and aspartate concentrations associated with an antiepileptogenic effect[1].
Cas No.
1078166-57-0
分子式
C23H20FNO5
分子量
409.413
别名
PF 04418948;PF04418948
储存和溶解度
DMSO:40.9 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years