MK-0524

MK-0524 is a potent, selective prostaglandin D2 (PGD2) receptor DP1 antagonist with Ki values of 0.57 nM and 0.75 µM for the DP1 and DP2 receptors, respectively. It inhibits PGD2-induced accumulation of cAMP in both washed platelets and platelet-rich plasma with IC50 values of 0.09 and 4.0 nM, respectively. In a sheep model of allergic rhinitis, 0.1 mg/kg MK-0524 completely blocked PGD2-induced nasal congestion. At a dose of 4 mg/kg, MK-0524 suppressed a nicotinic acid-induced vasodilatory response by 80% in a mouse model of flushing, an undesirable side-effect of niacin treatment for dyslipidemia. In an in vitro model of amyotrophic lateral sclerosis, MK-0524 has been shown to partially protect cultured motor neurons from PGD2-induced toxicity.Formal Name: (3R)-4-[(4-chlorophenyl)methyl]-7-fluoro-1,2,3,4-tetrahydro-5-(methylsulfonyl)-cyclopent[b]indole-3-acetic acid. CAS Number: 571170-77-9. Synonyms: Laropiprant. Molecular Formula: C21H19ClFNO4S. Formula Weight: 435.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 5 mg/ml. lambdamax: 222, 243, 311 nm. SMILES: FC1=CC2=C(N(CC3=CC=C(Cl)C=C3)C4=C2CC[C@@H]4CC(O)=O)C(S(C)(=O)=O)=C1. InChi Code: InChI=1S/C21H19ClFNO4S/c1-29(27,28)18-10-15(23)9-17-16-7-4-13(8-19(25)26)20(16)24(21(17)18)11-12-2-5-14(22)6-3-12/h2-3,5-6,9-10,13H,4,7-8,11H2,1H3,(H,25,26)/t13-/m1/s1. InChi Key: NXFFJDQHYLNEJK-CYBMUJFWSA-N.