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UNII:76LB1G2X6V

Names

[ CAS No. ]:
115104-28-4

[ Name ]:
UNII:76LB1G2X6V

[Synonym ]:
3-[({3-[(E)-2-(7-Chloroquinolin-2-yl)vinyl]phenyl}{[3-(dimethylamino)-3-oxopropyl]sulfanyl}methyl)sulfanyl]propanoic acid
mk-571,na salt
Propanoic acid, 3-[[[3-[(E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl][[3-(dimethylamino)-3-oxopropyl]thio]methyl]thio]-
mk-571 sodium salt
3-[({3-[(E)-2-(7-Chloro-2-quinolinyl)vinyl]phenyl}{[3-(dimethylamino)-3-oxopropyl]sulfanyl}methyl)sulfanyl]propanoic acid
mk-571 na
UNII:76LB1G2X6V

Biological Activity

[Description]:

MK-571 (L-660711) is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 is also a MRP4 and ABCC1 (MRP1) inhibitor. MK-571 inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release[1][2][3].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Leukotriene Receptor
Signaling Pathways >> GPCR/G Protein >> LPL Receptor
Research Areas >> Inflammation/Immunology

[Target]

LTD4:0.22 nM (Ki, In guinea pig lung)

LTD4:2.1 nM (Ki, In human lung)

LTD4:10.5 (pA2, on guinea pig ileum)

LTE4:10.4 (pA2, on guinea pig ileum)


[References]

[1]. Jones TR, et al. Pharmacology of L-660,711 (MK-571): a novel potent and selective leukotriene D4 receptor antagonist. Can J Physiol Pharmacol. 1989 Jan;67(1):17-28.  

[2]. Hara Y, et al. Inhibition of MRP4 prevents and reverses pulmonary hypertension in mice. J Clin Invest. 2011 Jul;121(7):2888-97.  

[3]. Mitra P, et al. Role of ABCC1 in export of sphingosine-1-phosphate from mast cells. Proc Natl Acad Sci U S A. 2006 Oct 31;103(44):16394-9.  

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
712.3±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C26H27ClN2O3S2

[ Molecular Weight ]:
515.09

[ Flash Point ]:
384.6±32.9 °C

[ Exact Mass ]:
514.115173

[ PSA ]:
121.10000

[ LogP ]:
5.93

[ Vapour Pressure ]:
0.0±2.4 mmHg at 25°C

[ Index of Refraction ]:
1.687

[ Storage condition ]:
20°C

Safety Information

[ Hazard Codes ]:
Xn

[ Risk Phrases ]:
36/37/38

[ Safety Phrases ]:
26-36/37

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds