LAROPIPRANT
| 中文名称 | LAROPIPRANT |
|---|---|
| 中文同义词 | 拉罗皮兰;拉罗皮兰,MK0524;(R)-2-(4-(4-氯苄基)-7-氟-5-(甲基磺酰基)-1,2,3,4-四氢环戊烷并[B]吲哚-3-基)乙酸;各拉西酮;拉罗匹仑;(R)-2-(4-(4-氯苄基)-7-氟-5-(甲基磺酰基)-1,2,3,4-四氢环戊二烯并[B]吲哚-3-基)乙酸;拉波普兰特;化合物 LAROPIPRANT |
| 英文名称 | MK 0524 |
| 英文同义词 | Cyclopent[b]indole-3-acetic acid, 4-[(4-chlorophenyl)methyl]-7-fluoro-1,2,3,4-tetrahydro-5-(methylsulfonyl)-, (3R)-Laropiprant;MK 0524;Laropiprant;MK-0524(Laropiprant)/;Laropiprant(MK0524);(3R)-4-[(4-Chlorophenyl)methyl]-7-fluoro-1,2,3,4-tetrahydro-5-(methylsulfonyl)cyclopent[b]indole-3-acetic acid;[(3R)-4-(4-chlorobenzyl)-7-fluoro-5-(Methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]acetic acid;(R)-2-(4-(4-chlorobenzyl)-7-fluoro-5-(Methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid |
| CAS号 | 571170-77-9 |
| 分子式 | C21H19ClFNO4S |
| 分子量 | 435.9 |
| EINECS号 | 682-424-1 |
| 相关类别 | G蛋白偶联受体&G蛋白;抗体-二抗;信号转导通路激酶抑制剂 |
| Mol文件 | 571170-77-9.mol |
| 结构式 |  |
LAROPIPRANT 性质
| 熔点 | 175∶C |
|---|---|
| 沸点 | 710.0±60.0 °C(Predicted) |
| 密度 | 1.48 |
| 储存条件 | Sealed in dry,Store in freezer, under -20°C |
| 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) |
| 酸度系数(pKa) | 4.54±0.10(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至米白色 |
| InChIKey | NXFFJDQHYLNEJK-CYBMUJFWSA-N |
| SMILES | OC(C[C@@H](CC1)C2=C1C3=CC(F)=CC(S(C)(=O)=O)=C3N2CC4=CC=C(C=C4)Cl)=O |
|
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.
安全信息
| WGK Germany | WGK 3 |
|---|---|
| 存储类别 | 11 - 可燃固体 |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025/12/22 | HY-50175 | Laropiprant | 571170-77-9 | 1 mg | 279元 |
| 2025/12/22 | HY-50175 | LAROPIPRANT Laropiprant | 571170-77-9 | 10mM * 1mLin DMSO | 589元 |