MK-7246

MK-7246 is an antagonist of the prostaglandin D2 (PGD2, Cay-12010) receptor CRTH2/DP2 (Ki = 2.5 nM). It is selective for CRTH2/DP2 over DP1, the PGF2alpha 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.Formal Name: (7R)-7-[[(4-fluorophenyl)sulfonyl]methylamino]-6,7,8,9-tetrahydro-pyrido[1,2-a]indole-10-acetic acid. CAS Number: 1218918-62-7. Molecular Formula: C21H21FN2O4S. Formula Weight: 416.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 50 mg/ml. SMILES: OC(CC1=C2N(C[C@@H](CC2)N(C)S(=O)(C3=CC=C(C=C3)F)=O)C4=CC=CC=C41)=O. InChi Code: InChI=1S/C21H21FN2O4S/c1-23(29(27,28)16-9-6-14(22)7-10-16)15-8-11-20-18(12-21(25)26)17-4-2-3-5-19(17)24(20)13-15/h2-7,9-10,15H,8,11-13H2,1H3,(H,25,26)/t15-/m1/s1. InChi Key: JTCAGRAKUAAYDY-OAHLLOKOSA-N.