(E)-3-[[[3-[2-(7-CHLORO-2-QUINOLINYL)ETHENYL]PHENYL]-[[(3-DIMETHYLAMINO)-3-OXOPROPYL]THIO]METHYL]THIO]-PROPANOIC ACID, SODIUM SALT

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 K_i 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

A receptor antagonist for the treatment of respiratory diseases. Cysteinyl leukotriene receptor antagonist MK-571 alters bronchoalveolar lavage fluid proteome in asthma.

Definition

ChEBI: MK 571 is a member of quinolines.

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.

storage

Store at -20°C

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