WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 524179
CAS#: 1175526-27-8 (free acid)
Description: AM-211 is a novel and potent antagonist of the prostaglandin D2 receptor type 2. 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 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.
MedKoo Cat#: 524179
CAS#: 1175526-27-8 (free acid)
Chemical Formula: C27H27F3N2O4
Exact Mass: 500.19229
Molecular Weight: 500.51
Elemental Analysis: C, 64.79; H, 5.44; F, 11.39; N, 5.60; O, 12.79
Synonym: AM-211; AM211; AM 211.
IUPAC/Chemical Name: 2-(2'-((3-benzyl-1-ethylureido)methyl)-6-methoxy-4'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl)acetic acid
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)
SMILES Code: O=C(O)CC1=CC(C2=CC=C(C(F)(F)F)C=C2CN(CC)C(NCC3=CC=CC=C3)=O)=C(OC)C=C1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 500.51 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Bain G, King CD, Brittain J, Hartung JP, Dearmond I, Stearns B, Truong YP, Hutchinson JH, Evans JF, Holme K. Pharmacodynamics, pharmacokinetics, and safety of AM211: a novel and potent antagonist of the prostaglandin D2 receptor type 2. J Clin Pharmacol. 2012 Oct;52(10):1482-93. Epub 2011 Nov 22. PubMed PMID: 22110163.
2: Bain G, Lorrain DS, Stebbins KJ, Broadhead AR, Santini AM, Prodanovich P, Darlington J, King CD, Lee C, Baccei C, Stearns B, Troung Y, Hutchinson JH, Prasit P, Evans JF. 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. doi: 10.1124/jpet.111.180430. Epub 2011 Apr 12. PubMed PMID: 21487069.
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.