AM211

SKU: orb1299624

Description

AM211 free acid is a potent, orally bioavailable small molecule antagonist of the prostaglandin D2 receptor DP2. It is a valuable research tool for investigating the role of the DP2 receptor in allergic and inflammatory diseases, suitable for both in vitro binding assays and in vivo pharmacological studies.

Research Area

Immunology & Inflammation, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1175526-27-8
• MW: 500.51
• Purity: 98.00% (May vary between batches)
• Formula: C₂₇H₂₇F₃N₂O₄
• SMILES: CCN(Cc1cc(ccc1-c1cc(CC(O)=O)ccc1OC)C(F)(F)F)C(=O)NCc1ccccc1
• Target: Prostaglandin Receptor
• Solubility: DMSO:125 mg/mL (249.75 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.99 mM)

Bioactivity

• Target IC50:
  DP2 (rat):10.4 nM|DP2 (guinea pig):4.9 nM |DP2 (mouse):7.8 nM |DP2 (human):4.9 nM
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AM 211, AM211, AM-211, AM211 free acid, Prostaglandin Receptor, prostaglandin D2 receptor, ProstaglandinReceptor

Compound Identifiers

PubChem CID

44158492