MK 0524 Chemical Properties

Melting point:

175∶C

Boiling point:

710.0±60.0 °C(Predicted)

Density 

1.48

storage temp. 

Sealed in dry,Store in freezer, under -20°C

solubility 

DMSO:20.0(Max Conc. mg/mL);45.88(Max Conc. mM)
DMF:20.0(Max Conc. mg/mL);45.88(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.45(Max Conc. mM)
Ethanol:5.0(Max Conc. mg/mL);11.47(Max Conc. mM)

form 

Powder

pka

4.54±0.10(Predicted)

color 

White to off-white

MK 0524 Usage And Synthesis

Uses

Laropiprant 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].

Definition

ChEBI: Laropiprant is an indolyl carboxylic acid.

Biological Activity

MK-0524 is a potent and selective prostaglandin D2 (PGD2) receptor PTGDR (DP1) antagonist with inverse agonist activity (Ki = 570 pM/DP1, 2.95 nM/TP, 745 nM/DP2, >890 nM for EP1/2/3/4, FP and IP). MK-0524 inhibits cAMP accumulation in PGD2-challenged human platelets (IC50 = 90 pM) and blocks PGD2-induced nasal congestion in a sheep allergic rhinitis model in vivo (by 99% at 0.1 mg/kg i.v.). MK-0524 decreases DP1-dependent basal cAMP level in HEK293 (1-100 nM) without affecting DP1-dependent basal ERK1/2 phosphorylation (up to 1 μM).

in vivo

IC 50

DP: 0.57 nM (Ki); TP Receptor: 2.95 nM (Ki)

storage

Store at -20°C

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. DOI:10.1021/jm0603668
[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. DOI:10.1080/00498250601175565

MK 0524(571170-77-9)Related Product Information

• CYCLOPENT[B]INDOLE, 7-FLUORO-1,2,3,4-TETRAHYDRO-
• MK 0524