85-2072-51 DP2 Antagonist I (CRTH2 Antagonist I, GPR44 Antagonist I, (4-Chloro-2-((2-methyl-5-(propylsulfonyl)phenyl)ethynyl)phenoxy)acetic Acid) 2mg 217323
85-2072-51 DP2 Antagonist I (CRTH2 Antagonist I, GPR44 Antagonist I, (4-Chloro-2-((2-methyl-5-(propylsulfonyl)phenyl)ethynyl)phenoxy)acetic Acid) 2mg 217323
A cell-permeable alkynylphenoxyacetic acid that acts as a high affinity antagonist against the G protein-coupled PGD2 receptor CRTH2/DP2 (Ki = 2.0 and 2.4nM against 1.5nM PGD2 for human & murine DP2 binding, respectively), exhibiting much reduced potency against DP1 (Ki = 1.58uM; IC50 = 10uM), PGE receptor EP2 (54% inhibition at 10uM), and little or no activity toward 49 other receptors and ion channels. Effectively inhibits PGD2-induced cellular activation (IC50 = 32 and 80nM, respectively, using CHO-CRTH2 or human whole blood) in vitro and is efficacious in alleviating airway eosinophil infiltration in OVA-sensitized mice (30mg/kg; p.o.) in vivo with good oral bioavailability.
Synonyms:CRTH2 Antagonist I, GPR44 Antagonist I, (4-Chloro-2-((2-methyl-5-(propylsulfonyl)phenyl)ethynyl)phenoxy)acetic Acid
Molecular Formula:C₂₀H₁₉ClO₅S
Solubility:DMSO
Primary Target:DP2
Primary Target Ki:2nM
Molar Mass:406.88
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
