571170-77-9
571170-77-9 结构式
基本信息
各拉西酮
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
MK 0524
Cardaptive
Laropiprant
Laropiprant, >=99%
Laropiprant(MK0524)
MK-0524(Laropiprant)/
MK0524
LAROPIPRANT
MK-0524
[(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
物理化学性质
DMF:20.0(Max Conc. mg/mL);45.88(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.45(Max Conc. mM)
Ethanol:5.0(Max Conc. mg/mL);11.47(Max Conc. mM)
常见问题列表
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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.