Product Overview
Laropiprant (Cardaptive; MK 0524) is a potent, selective DP1 receptor antagonist with Ki values of 0.57 nM and 0.75 μM for the DP1 and DP2 receptors, respectively. Laropiprant (Cardaptive; MK 0524) inhibits PGD2-induced accumulation of cAMP in both washed platelets and platelet-rich plasma with IC50 values of 0.09 and 4.0 nM, respectively. In a sheep model of allergic rhinitis, 0.1 mg/kg MK 0524 completely blocked PGD2-induced nasal congestion. At a dose of 4 mg/kg, MK 0524 suppressed a nicotinic acid-induced vasodilatory response by 80% in a murine model of flushing, an undesirable side-effect of niacin treatment for dyslipidemia.
Synonyms
Cardaptive; MK 0524; MK-0524,Laropiprant
Molecular Formula
C21H19ClFNO4S
Chemical Name
2-[(3R)-4-[(4-chlorophenyl)methyl]-7-fluoro-5-methylsulfonyl-2,3-dihydro-1H-cyclopenta[b]indol-3-yl]acetic acid
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request