| Description | AM211 (AM211 free acid) is a potent and orally bioavailable antagonist of prostaglandin D2 (PGD2) receptor type 2 (DP2) |
| In vivo | 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]. |
| Target activity | DP2 (rat):10.4 nM, DP2 (mouse):7.8 nM , DP2 (guinea pig):4.9 nM , DP2 (human):4.9 nM |
| Synonyms | AM211 free acid |
| molecular weight | 500.51 |
| Molecular formula | C27H27F3N2O4 |
| CAS | 1175526-27-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 125 mg/mL (249.75 mM) |
| References | 1. Bain G , Lorrain D S , Stebbins K J , et al. Pharmacology of AM211, a Potent and Selective Prostaglandin D2 Receptor Type 2 Antagonist That Is Active in Animal Models of Allergic Inflammation[J]. Journal of Pharmacology and Experimental Therapeutics, 2011, 338(1):290-301. 2. Bain G , King C D , Brittain J , et al. Pharmacodynamics, Pharmacokinetics, and Safety of AM211: A Novel and Potent Antagonist of the Prostaglandin D2 Receptor Type 2[J]. The Journal of Clinical Pharmacology, 2012, 52(10). |