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AM211

Cat. No. M10632
AM211 Structure
Synonym:

AM-211; AM211 free acid

Size Price Availability
10mg USD 154  USD154 4-7 Days
50mg USD 590  USD590 4-7 Days
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Quality Control & Documentation
Biological Activity

AM-211 is a novel and potent antagonist of the prostaglandin D2 receptor type 2, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively. AM-211 is active in animal models of allergic inflammation. AM211 has high affinity for human, mouse, rat, and guinea pig DP2 and it shows selectivity over other prostanoid receptors and enzymes. 

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 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.

Chemical Information
Molecular Weight 500.51
Formula C27H27F3N2O4
CAS Number 1175526-27-8
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] G Bain, et al. J Clin Pharmacol . Pharmacodynamics, pharmacokinetics, and safety of AM211: a novel and potent antagonist of the prostaglandin D2 receptor type 2

[2] Gretchen Bain, et al. J Pharmacol Exp Ther . Pharmacology of AM211, a potent and selective prostaglandin D2 receptor type 2 antagonist that is active in animal models of allergic inflammation

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Keywords: AM211, AM-211; AM211 free acid supplier, Prostaglandin Receptor, inhibitors, activators


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