DP2 Antagonist I (CRTH2 Antagonist I, GPR44 Antagonist I, (4-Chloro-2-((2-methyl-5-(propylsulfonyl)phenyl)ethynyl)phenoxy)acetic Acid)
Artikelnummer:
USB-217323
Hersteller Artikelnummer:
217323
Alternativnummer:
USB-217323-2
Hersteller:
US Biological
Kategorie:
Biochemikalien
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 4C. For long-term storage, aliquot and store at 4C. 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.
Molekulargewicht:
406.88
Reinheit:
98% (HPLC)
Formulierung:
Supplied as a white powder.
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