572874-50-1

572874-50-1 structure

Name: MK 0524 sodium salt
Chemical Name: Sodium [(3R)-4-(4-chlorobenzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3 ,4-tetrahydrocyclopenta[b]indol-3-yl]acetate
CAS Number: 572874-50-1
Molecular Formula: C₂₁H₁₈ClFNNaO₄S
Molecular Weight: 457.87800
Catalog: Signaling Pathways GPCR/G Protein Prostaglandin Receptor
Create Date: 2016-06-12 14:54:50
Modify Date: 2024-01-09 17:18:13
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].

Name	Sodium [(3R)-4-(4-chlorobenzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3 ,4-tetrahydrocyclopenta[b]indol-3-yl]acetate

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.