ChemicalBook Product Catalog Biochemical Engineering Biochemical Reagents Agonist Inhibitors (E)-3-[[[3-[2-(7-CHLORO-2-QUINOLINYL)ETHENYL]PHENYL]-[[(3-DIMETHYLAMINO)-3-OXOPROPYL]THIO]METHYL]THIO]-PROPANOIC ACID, SODIUM SALT

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

Product Name(E)-3-[[[3-[2-(7-CHLORO-2-QUINOLINYL)ETHENYL]PHENYL]-[[(3-DIMETHYLAMINO)-3-OXOPROPYL]THIO]METHYL]THIO]-PROPANOIC ACID, SODIUM SALT
CAS115104-28-4
MFC26H27ClN2O3S2
MW515.09
EINECS
MOL File115104-28-4.mol

Chemical Properties

Melting point	65-70°C
Boiling point	712.3±60.0 °C(Predicted)
Density	1.327±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	Soluble in DMSO (up to 50 mg/ml).
pka	4.27±0.10(Predicted)
form	Off-white solid.
color	Yellow
Stability	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
InChIKey	AXUZQJFHDNNPFG-UXBLZVDNSA-N
SMILES	S(C(SCCC(=O)O)c1cc(ccc1)\C=C\c2nc3c(cc2)ccc(c3)Cl)CCC(=O)N(C)C

Safety Information

WGK Germany	WGK 1
Storage Class	11 - Combustible Solids

Usage And Synthesis

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] T R JONES. Pharmacology of L-660,711 (MK-571): a novel potent and selective leukotriene D4 receptor antagonist.[J]. Canadian journal of physiology and pharmacology, 1989, 67 1: 17-28. DOI:10.1139/y89-004
[2] DENIS J DUPRÉ. Inverse agonist activity of selected ligands of the cysteinyl-leukotriene receptor 1.[J]. Journal of Pharmacology and Experimental Therapeutics, 2004, 309 1: 102-108. DOI:10.1124/jpet.103.059824
[3] E VELLENGA. Interleukin-6 production by activated human monocytic cells is enhanced by MK-571, a specific inhibitor of the multi-drug resistance protein-1.[J]. British Journal of Pharmacology, 1999, 127 2: 441-448. DOI:10.1038/sj.bjp.0702577

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

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

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