Laropiprant

Product Description

Laropiprant is a potent and selective prostaglandin D₂ receptor antagonist (IC₅₀ = 0.09 nM in washed platelets; K_i = 0.57). It exhibits selectivity for binding to PGD₂ receptors over other prostanoid receptors (K_i values are ≥ 2.95 nM for TP, EP₁, EP₂, EP₃, EP₄, FP and IP). Laropiprant promotes coagulation of whole blood ex vivo and reduces bleeding time in mice in vivo. In a mouse model of intracerebral hemorrhage, Laropiprant reduces lesion volume and attenuates neurological deficit scores. The compound also reduces Niacin (Cat. No. 4106) induced vasodilation.

Solubility

Preparing Stock Solutions for Laropiprant

The following data is based on the product molecular weight 435.90

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.29 mL	11.47 mL	22.94 mL
5 mM	0.46 mL	2.29 mL	4.59 mL
10 mM	0.23 mL	1.15 mL	2.29 mL
50 mM	0.05 mL	0.23 mL	0.46 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Kong Niacin promotes cardiac healing after myocardial infarction through activation of the myeloid prostaglandin D₂ receptor subtype 1. J.Pharmacol.Exp.Ther. 2017 PMID: 28057839
• Ahmad Efficacy of Laropiprant in minimizing brain injury following experimental intracerebral hemorrhage. Sci.Rep. 2017 PMID: 28842638
• Sturino 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 PMID: 17300164