AM211 是可口服的选择性前列腺素受体拮抗剂,对人、小鼠、豚鼠和大鼠的 DP2 的IC50值分别为 4.9、7.8、4.9 和 10.4 nM。
产品描述
AM211 is a potent and orally bioavailable antagonist of prostaglandin D2 (PGD2) receptor type 2 (DP2)
体内活性
AM211 exhibits good oral bioavailability in rats and dogs and dose-dependently inhibits 13,14-dihydro-15-keto-PGD(2)-induced leukocytosis in a guinea pig pharmacodynamic assay. AM211 demonstrates efficacy in two animal models of allergic inflammation, including an ovalbumin-induced lung inflammation model in guinea pigs and an ovalbumin-induced mouse model of allergic rhinitis. AM211 represents a potent and selective antagonist of DP2 that may be used clinically to evaluate the role of DP2 in T helper 2-driven allergic inflammatory diseases[1].
Cas No.
1175526-27-8
分子式
C27H27F3N2O4
分子量
500.518
别名
AM211 free acid
储存和溶解度
DMSO:125 mg/mL (249.75 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years