MK-571 (sodium salt)

MK-571 is a cysteinyl leukotriene 1 (CysLT1) receptor antagonist (Ki = 2.1 nM in a radioligand binding assay using isolated human lung membranes). It inhibits contractions induced by leukotriene D4 (LTD4, Cay-20310) or LTE4 (Cay-20410) in histamine-primed isolated guinea pig trachea (pA2s = 9.4 and 9.1, respectively), but does not inhibit contractions induced by LTC4 (Cay-20210) in histamine-primed isolated guinea pig trachea when used at a concentration of 190 nM. MK-571 (100 nM) inhibits LTD4-induced calcium mobilization in COS-7 monkey kidney cells expressing the human CysLT1 receptor in a reporter assay. MK-571 (5 mg/kg) improves tissue damping and elasticity, markers of lung function, and decreases IL-4 and IL-5 levels in bronchoalveolar lavage fluid (BALF) in a mouse model of ovalbumin-induced asthma.Formal Name: (E)-3-[[[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl][[3-(dimethylamino)-3-oxopropyl]thio]methyl]thio]-propanoic acid, sodium salt. CAS Number: 115103-85-0. Synonyms: L-660,711. Molecular Formula: C26H26ClN2O3S2 . Na. Formula Weight: 537.1. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, Ethanol: 1 mg/ml, H20: 20 mg/ml, PBS (pH 7.2): 10 mg/ml. lambdamax: 226, 283, 328, 345, 358 nm. SMILES: ClC1=CC(N=C(/C=C/C2=CC(C(SCCC(N(C)C)=O)SCCC([O-])=O)=CC=C2)C=C3)=C3C=C1.[Na+]. InChi Code: InChI=1S/C26H27ClN2O3S2.Na/c1-29(2)24(30)12-14-33-26(34-15-13-25(31)32)20-5-3-4-18(16-20)6-10-22-11-8-19-7-9-21(27)17-23(19)28-22,/h3-11,16-17,26H,12-15H2,1-2H3,(H,31,32),/q,+1/p-1/b10-6+,. InChi Key: XNAYQOBPAXEYLI-AAGWESIMSA-M.