MK-0524
MK-0524 is a specific prostaglandin D2 receptor (DP1) inhibitor that functions as an inverse agonist. MK-0524 decreases niacin-induced flushing during niacin treatment of dyslipidemia and is most often studied in combination with niacin. The ability of MK-0524 to inhibit DP1 prevents PGD2-induced hyaluron synthesis, yielding beneficial results in preventing pathological changes associated with thyroid eye disease. This compound also has antithrombotic activity, displaying weak inhibitory action against the thromboxane A2 receptor, inhibiting platelet activation at high concentrations.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18945307
| Cas No. |
571170-77-9 |
|---|---|
| Purity |
≥99% |
| Formula |
C21H19ClFNO4S |
| Formula Wt. |
435.90 |
| IUPAC Name |
2-[(3R)-4-[(4-chlorophenyl)methyl]-7-fluoro-5-methylsulfonyl-2,3-dihydro-1H-cyclopenta[b]indol-3-yl]acetic acid |
| Synonym |
Laropiprant |
| Melting Point |
178.6°C |
| Appearance |
White to off white powder |
Labrecque P, Roy SJ, Fréchette L, et al. Inverse agonist and pharmacochaperone properties of MK-0524 on the prostanoid DP1 receptor. PLoS One. 2013 Jun 10;8(6):e65767. PMID: 23762421.
Philipose S, Konya V, Lazarevic M, et al. Laropiprant attenuates EP3 and TP prostanoid receptor-mediated thrombus formation. PLoS One. 2012;7(8):e40222. PMID: 22870195.
Guo N, Baglole CJ, OLoughlin CW, et al. Mast cell-derived prostaglandin D2 controls hyaluronan synthesis in human orbital fibroblasts via DP1 activation: implications for thyroid eye disease. J Biol Chem. 2010 May 21;285(21):15794-804. PMID: 20308056.
Luo WL, Crumley T, Ebel D, et al. Single therapeutic and supratherapeutic doses of laropiprant, a selective prostaglandin D2 receptor 1 antagonist, do not prolong the QTcF interval in healthy volunteers. J Clin Pharmacol. 2010 Nov;50(11):1273-9. PMID: 20107202.
Paolini JF, Bays HE, Ballantyne CM, et al. Extended-release niacin/laropiprant: reducing niacin-induced flushing to better realize the benefit of niacin in improving cardiovascular risk factors. Cardiol Clin. 2008 Nov;26(4):547-60. PMID: 19031552.
