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|300264-2MG||Glass bottle||2 mg||
|Overview||A cell-permeable alkynylphenoxyacetic acid that acts as a high affinity antagonist against the G protein-coupled PGD2 (Cat. No. 538909) receptor CRTH2/DP2 (Ki = 2.0 and 2.4 nM against 1.5 nM PGD2 for human & murine DP2 binding, respectively), exhibiting much reduced potency against DP1 (Ki = 1.58 µM; IC50 = 10 µM), PGE receptor EP2 (54% inhibition at 10 µM), and little or no activity toward 49 other receptors and ion channels. Effectively inhibits PGD2-induced cellular activation (IC50 = 32 and 80 nM, respectively, using CHO-CRTH2 or human whole blood) in vitro and is efficacious in alleviating airway eosinophil infiltration in OVA- (Cat. No. 32467) sensitized mice (30 mg/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|
|References||Crosignani, S., et al. 2011. J Med Chem. 54, 7299.|
|Structure formula Image|
|Primary Target K<sub>i</sub>||2 nM|
|Purity||≥98% by HPLC|
|Safety Information according to GHS|
|Product Usage Statements|
|Packaged under inert gas||Packaged under inert gas|
|Crosignani, S., et al. 2011. J Med Chem. 54, 7299.|
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.