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MK 0524 sodium salt

Names

[ CAS No. ]:
572874-50-1

[ Name ]:
MK 0524 sodium salt

Biological Activity

[Description]:

Laropiprant sodium is a potent and selective DP receptor antagonist with Ki values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively[1][2][3].

[Related Catalog]:

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

[Target]

TP:2.95 nM (Ki)

DP/DP1 Receptor:0.57 nM (Ki)


[In Vitro]

Laropiprant sodium (0.01-1000 μM; 10 mins; HEK293 cells) is an Inverse Agonist of DP1 cAMP Signaling and reduces DP1 cAMP signaling below basal levels[1]. Laropiprant sodium (1 μM; 0-24 h; HEK293 cells) is a pharmacochaperone in promoting DP1 cell surface expression[1].

[References]

[1]. Labrecque P, et, al. Inverse agonist and pharmacochaperone properties of MK-0524 on the prostanoid DP1 receptor. PLoS One. 2013 Jun 10;8(6):e65767.

[2]. Sturino CF, et, al. Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524). J Med Chem. 2007 Feb 22;50(4):794-806.

[3]. Chang SW, et, al. The pharmacokinetics and disposition of MK-0524, a Prosglandin D2 Receptor 1 antagonist, in rats, dogs and monkeys. Xenobiotica. 2007 May;37(5):514-33.

Chemical & Physical Properties

[ Molecular Formula ]:
C21H18ClFNNaO4S

[ Molecular Weight ]:
457.87800

[ Exact Mass ]:
457.05300

[ PSA ]:
87.58000

[ LogP ]:
4.13620

Related Compounds