AM211

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AM211 是一种有效的口服生物可利用的 2 型前列腺素 D2 (PGD2) 受体 (DP2) 拮抗剂。

AM211 is a potent and orally bioavailable antagonist of prostaglandin D2 (PGD2) receptor type 2 (DP2).

AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively. In the presence of 0.2% serum albumin, AM211 inhibits radiolabeled PGD2 binding to human, mouse, guinea pig, and rat DP2 with IC50 values of 12.2, 20.1, 22.9, and 34.2 nM, respectively. AM211 displays high selectivity for DP2 versus other receptors in the prostanoid family, with IC50 values for the inhibition of radioligand binding to human TP, IP, DP1, and FP of more than 100 μM. AM211 (100 μM) shows no activity at COX-1, COX-2 enzymes as well as PPAR family of nuclear receptors.

AM211 (1, 10, and 30 mg/kg, p.o.) dose-dependently decreases in the number of DK-PGD2-induced peripheral blood leukocytes, with a calculated ED50 of 0.85 mg/kg. AM211 (30 mg/kg) also decreases antigen-induced pulmonary inflammation in guinea pigs. AM211 (10 mg/kg, p.o.) causes significant decrease in ovalbumin (OVA)-induced sneezing in a mouse model of allergic rhinitis.

AM211 free acid

GPCR/G Protein

Prostaglandin Receptor

prostaglandin D2 receptor

——

——

1175526-27-8

500.51

C27H27F3N2O4

>98% (HPLC)

DMSO:125 mg/mL (249.75 mM)

CCN(Cc1cc(C(F)(F)F)ccc1-c1cc(CC(=O)O)ccc1OC)C(=O)NCc1ccccc1

——

(-20℃)

With Ice Pack

≥ 2 years