LAS191859

LAS191859 is a potent antagonist of CRTH2/DP2 with IC50 values of 9.58, 14, 15.5, and 7.6 nM for recombinant human, rat, mouse, and guinea pig CRTH2/DP2 receptors, respectively. It is selective for CRTH2/DP2 over a panel of 65 enzymes, ion channels, and transporters with 50s = 2 and 8.2 nM in isolated eosinophils and whole blood, respectively) and eosinophil chemotaxis (IC50 = 1.3 nM) induced by prostaglandin D2 (PGD2, Cay-12010) binding to CRTH2/DP2. Oral administration of LAS191859 reduces PGD2-induced systemic eosinophilia in guinea pigs (ID50 = 131 µg/kg).Formal Name: 1-[2-[[(cyclopropylcarbonyl)ethylamino]methyl]-4-(trifluoromethyl)phenyl]-6-methyl-1H-pyrrolo[2,3-b]pyridine-3-acetic acid. CAS Number: 1420071-13-1. Molecular Formula: C24H24F3N3O3. Formula Weight: 459.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml, Ethanol: 2.5 mg/ml. lambdamax: 272 nm. SMILES: CCN(C(C1CC1)=O)CC2=CC(C(F)(F)F)=CC=C2N3C=C(CC(O)=O)C4=C3N=C(C)C=C4. InChi Code: InChI=1S/C24H24F3N3O3/c1-3-29(23(33)15-5-6-15)12-17-10-18(24(25,26)27)7-9-20(17)30-13-16(11-21(31)32)19-8-4-14(2)28-22(19)30/h4,7-10,13,15H,3,5-6,11-12H2,1-2H3,(H,31,32). InChi Key: KGBYKYDRYYERIX-UHFFFAOYSA-N.