产品描述:
MK-7246 is an antagonist of the prostaglandin D2 (PGD2; Item No. 12010) receptor CRTH2/DP2 (Ki = 2.5 nM).{61486} It is selective for CRTH2/DP2 over DP1, the PGF2α receptor (FP), the PGI2 receptor (IP), and the thromboxane A2 (TP) receptor (Kis = 373, >25,100, >23,030, and 3,804 nM, respectively), as well as the PGE2 receptor subtypes 1-4 (EP1-4; Kis = 7,668-23,330 nM). MK-7246 inhibits 13,14-dihydro-15-keto-PGD2-induced inhibition of cAMP formation in HEK293 cells expressing human CRTH2/DP2 (IC50 = 3 nM). It also inhibits 13,14-dihydro-15-keto-PGD2-induced eosinophil shape change (IC50 = 2.2 nM) and CD11b upregulation on eosinophils and basophils in isolated human whole blood (IC50s = 6.2 and 5.4 nM, respectively). MK-7246 (1 mg/kg) decreases antigen-induced late-phase bronchoconstriction and completely prevents airway hyperresponsiveness in sheep.