AM211 is a potent, selective, orally bioavailable prostaglandin receptor (DP2) antagonist (inhibitor) with IC50s of 4.9 nM, 7.8 nM, and 4.9 nM for human, mouse, guinea pig, and rat DP2, respectively. 10.4 nM.

Physicochemical Properties

Molecular Formula	C27H27N2O4F3
Molecular Weight	500.50948
Exact Mass	500.192
CAS #	1175526-27-8
Related CAS #	1175526-27-8 (free acid);1263077-74-2 (sodium);
PubChem CID	44158492
Appearance	White to off-white solid powder
LogP	5.944
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	9
Heavy Atom Count	36
Complexity	714
Defined Atom Stereocenter Count	0
InChi Key	OPXIRFWNLBDKQB-UHFFFAOYSA-N
InChi Code	InChI=1S/C27H27F3N2O4/c1-3-32(26(35)31-16-18-7-5-4-6-8-18)17-20-15-21(27(28,29)30)10-11-22(20)23-13-19(14-25(33)34)9-12-24(23)36-2/h4-13,15H,3,14,16-17H2,1-2H3,(H,31,35)(H,33,34)
Chemical Name	2-[3-[2-[[benzylcarbamoyl(ethyl)amino]methyl]-4-(trifluoromethyl)phenyl]-4-methoxyphenyl]acetic acid
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	AM211 is an oral bioavailable, powerful, selective prostaglandin D2 (PGD2) type 2 receptor (DP2) antagonist. Its IC50 for DP2 in humans, mice, guinea pigs, and rats is 4.9 nM. 4.9 nM, 10.4 nM, 7.8 nM. In the presence of 0.2% serum albumin, AM211 inhibits the binding of radiolabeled PGD2 to human, mouse, guinea pig, and rat DP2 with IC50 values of 12.2, 20.1, 22.9, and 34.2 nM, respectively. AM211 has superior selectivity for DP2 as compared to other prostaglandin family receptors. It also inhibits radioligand binding to human TP, IP, DP1, and FP, with IC50 values higher than 100 μM. AM211 (100 μM) exhibits no effect against the PPAR nuclear receptor family, COX-1, or COX-2 enzymes [1].
ln Vivo	AM211 (1, 10 and 30 mg/kg, orally) dose-dependently reduced DK-PGD2-induced peripheral blood leukocyte counts with an estimated ED50 of 0.85 mg/kg. AM211 (30 mg/kg) also decreases antigen-induced lung inflammation in guinea pigs. AM211 (10 mg/kg, orally) effectively lowers ovalbumin (OVA)-induced sneeze in a mouse model of allergic rhinitis [1].
References	[1]. Pharmacology of AM211, a potent and selective prostaglandin D2 receptor type 2 antagonist that is active in animal models of allergic inflammation. J Pharmacol Exp Ther. 2011 Jul;338(1):290-301.

Solubility Data

Solubility (In Vitro)

DMSO : ≥ 125 mg/mL (~249.75 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (4.16 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (4.16 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with heating and sonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.08 mg/mL (4.16 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.9980 mL	9.9898 mL	19.9796 mL
	5 mM	0.3996 mL	1.9980 mL	3.9959 mL
	10 mM	0.1998 mL	0.9990 mL	1.9980 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.