| Description | Laropiprant (MK-0524) is a potent and selective antagonist of prostaglandin D2 (PGD2) receptor (DP) such as and DP/DP1 receptor(Ki = 0.57 nM) and TP Receptor(Ki = 2.95 nM). |
| In vitro | Laropiprant blocks DP receptor-dependent enhance in VASP phosphorylation, as well as inhibition of P-selectin expression, GPIIb/IIIa activation, and in vitro thrombus formation. Laropiprant antagonizes the increased platelet aggregation by TP and EP3 receptor activation. Laropiprant (1 μM) induces a significant inhibition of the aggregation but still counteracts the pronounced inhibition caused by PGD2 (30 nM) and BW245c (3 nM). Laropiprant (10 μM) and niacin inhibit in vitro thrombus formation[2]. |
| Target activity | DP/DP1 receptor:0.57 nM (ki), TP receptor:2.95 nM (ki) |
| Synonyms | MK-0524 |
| molecular weight | 435.9 |
| Molecular formula | C21H19ClFNO4S |
| CAS | 571170-77-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 100 mg/mL (229.41 mM) |
| References | 1. 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. 2. Philipose S, et al. Laropiprant Attenuates EP3 and TP Prostanoid Receptor-Mediated Thrombus Formation. PLoS One. 2012;7(8):e40222. |