115104-28-4 Usage
Description
MK-571 is a selective, orally active CysLT1 receptor antagonist. It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively, which is indicative of CysLT1 receptor-mediated activity in these preparations. MK-571 effectively blocks LTD4 activation of recombinant human and murine CysLT1 receptors but is ineffective at blocking LTC4 or LTD4 activation of the recombinant human or murine CysLT2 receptors.
Chemical Properties
Yellow Solid
Uses
Different sources of media describe the Uses of 115104-28-4 differently. You can refer to the following data:
1. A receptor antagonist for the treatment of respiratory diseases. Cysteinyl leukotriene receptor antagonist MK-571 alters bronchoalveolar lavage fluid proteome in asthma.
2. A receptor antagonist for the treatment of respiratory diseases. Cysteinyl leukotriene receptor antagonist MK-571 alters bronchoalveolar lavage fluid proteome in asthma
Biological Activity
Potent CysLT 1 (LTD 4 ) leukotriene receptor inverse agonist (EC 50 = 1.3 nM). Antagonizes LTD 4 -induced contractions of guinea pig trachea and ileum (pA 2 values are 9.4 and 10.5 respectively). Also inhibitor of multidrug resistance protein-1 (MRP1) mediated transport; in vitro augments the effects of cytotoxic agents on malignant cells.
References
1) Jones et al. (1989) Pharmacology of L-660,711 (MK-571): a novel potent and selective leukotriene D4 receptor antagonist.; Can. J. Physiol. Pharmacol. 67, 17
2) Dupre et al. (2004) Inverse agonist activity of selected ligands of the cysteinyl-leukotriene receptor 1; J. Pharmacol. Exp. Ther. 309 102
3) Vellenga et al. (1999) Interleukin-6 production by activated human monocytic cells is enhanced by MK-571, a specific inhibitor of the multi-drug resistance protein-1; Br .J. Pharmacol. 127 441
Check Digit Verification of cas no
The CAS Registry Mumber 115104-28-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,1,5,1,0 and 4 respectively; the second part has 2 digits, 2 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 115104-28:
(8*1)+(7*1)+(6*5)+(5*1)+(4*0)+(3*4)+(2*2)+(1*8)=74
74 % 10 = 4
So 115104-28-4 is a valid CAS Registry Number.
InChI:InChI=1/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+;
115104-28-4Relevant articles and documents
ASYMMETRIC DITHIOACETALS III: THE PREPARATION OF THE ENANTIOMERS OF 3-((((3-(2-(7-CHLOROQUINOLIN-2-YL)-(E)-ETHENYL)PHENYL)-3-DIMETHYLAMINO-3-OXOPROPYLTHIO)METHYL)THIO)PROPIONIC ACID (L-660,711) (MK-571), AN ANTAGONIST OF LEUKOTRIENE D4
Young, Robert N.,Gauthier, Jacques Yves,Therien, Michel,Zamboni, Robert
, p. 967 - 978 (2007/10/02)
The application of a novel method for the preparation of chiral dithioacetals to the synthesis of the enantiomers of L-660,711, an antagonist of leukotriene D4, is described.Reaction of 3-(t-butyldiphenylsilyloxymethyl)benzaldehyde or isophthal
