Laropiprant 是DP receptor的选择性拮抗剂，Ki为 0.57 nM，对 TP 受体的Ki为 2.95 nM。

Laropiprant 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).

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].

571170-77-9

C21H19ClFNO4S

435.9

MK-0524

DMSO:100 mg/mL (229.41 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years