DP2 Antagonist I (CRTH2 Antagonist I, GPR44 Antagonist I, (4-Chloro-2-((2-methyl-5-(propylsulfonyl)phenyl)ethynyl)phenoxy)acetic Acid)

Size

£482.00

SKU:: 217323
Molecular Weight:: 406.88
Purity:: ≥98% (HPLC)
Storage Conditions:: 4°C
Supplier:: United States Biological
Format:: Supplied as a white powder.
Extra Details:: 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.