| 中文名称 | LAROPIPRANT |
| 英文名称 | MK 0524 |
| CAS号 | 571170-77-9 |
| 分子式 | C21H19ClFNO4S |
| 分子量 | 435.9 |
| EINECS号 | 682-424-1 |
| 熔点 | 175∶C |
| 沸点 | 710.0±60.0 °C(Predicted) |
| 密度 | 1.48 |
| 溶解度 | DMSO:20.0(最大浓度 mg/mL);45.88(最大浓度 mM)DMF:20.0(最大浓度 mg/mL);45.88(最大浓度 mM)DMSO:PBS ( pH 7.2) (1:1):0.5(最大浓度 mg/mL);1.45(最大浓度 mM)乙醇:5.0(最大浓度 mg/mL);11.47(最大浓度 mM) |
| 形态 | 粉末 |
| 酸度系数(pKa) | 4.54±0.10(Predicted) |
| 颜色 | 白色至米白色 |
|
DP/DP1 Receptor 0.57 nM (Ki) |
TP Receptor 2.95 nM (Ki) |
Laropiprant is a potent, selective DP receptor antagonist with K i values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively.. Laropiprant (1 µM) causes a significant inhibition of the aggregation but still counteractes the pronounced inhibition caused by PGD2 (30 nM) and BW245c (3 nM). Laropiprant blocks DP receptor-dependent increase 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 (10 µM) and niacin inhibit in vitro thrombus formation.
