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|300266-2MG||Glass bottle||2 mg||
|Overview||The (R) enantiomer of 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 = 5.3 and 5.0 nM against human & murine DP2, respectively), exhibiting much reduced potency against a panel of more than 50 other receptors and ion channels. Effectively inhibits DP2-dependent chemotaxis of primary human eosinophils (IC50 = 100 nM). Exhibits higher Caco-2 permeability than DP2 Antagonist I (Cat. No. 300264), but less oral bioavailability in mice.|
|Synonyms||CRTH2 Antagonist II, GPR44 Antagonist II, (R)-(5-Chloro-1'-(5-chloro-2-fluorobenzyl)-2,2',5'-trioxospiro(indole-3,3→-pyrrolidin)-1(2H)-yl)acetic acid|
|References||Crosignani, S., et al. 2008. J Med Chem. 51, 2227.|
|Structure formula Image|
|Primary Target K<sub>i</sub>||5.3 nM|
|Purity||≥93% by HPLC|
|Safety Information according to GHS|
|Product Usage Statements|
|Packaged under inert gas||Packaged under inert gas|
|Crosignani, S., et al. 2008. J Med Chem. 51, 2227.|
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.