Laropiprant

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Chemical Structure| 571170-77-9 同义名 : MK-0524
CAS号 : 571170-77-9
货号 : A411003
分子式 : C21H19ClFNO4S
纯度 : 99%+
分子量 : 435.896
MDL号 : MFCD11042421
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(240.88 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Prostaglandin D2 (PGD2) are one of the key mediators in allergic conditions, such as allergic rhinitis. Laropiprant is a potent, selective PGD2 receptor (DP) antagonist with a competition binding affinity constant (Ki) value of 0.57±0.71nM and a dissociation constant (Kd) value of 0.03nM. It inhibited PGD2-induced accumulation of cAMP in both washed platelets and platelet-rich plasma with IC50 values of 0.09nM and 4.0nM, respectively. In a sheep model of allergic rhinitis, laropiprant at a dose of 0.1mg/kg effectively blocked (99%) PGD2-induced nasal congestion[3]. In male C57BL/6 mice, pretreatment with laropiprant (0.004–4mg/kg, i.p.) inhibited nicotinic acid-induced vasodilation in a dose-dependent manner[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.29mL

0.46mL

0.23mL

11.47mL

2.29mL

1.15mL

22.94mL

4.59mL

2.29mL
参考文献

[1]HPS2-THRIVE Collaborative Group, Landray MJ, et al. Effects of extended-release niacin with laropiprant in high-risk patients. N Engl J Med. 2014 Jul 17;371(3):203-12.

[2]Philipose S, Konya V, et al. Laropiprant attenuates EP3 and TP prostanoid receptor-mediated thrombus formation. PLoS One. 2012;7(8):e40222.

[3]Sturino CF, O'Neill G, Lachance N, 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;50(4):794-806.

[4]Cheng K, Wu TJ, Wu KK, et al. Antagonism of the prostaglandin D2 receptor 1 suppresses nicotinic acid-induced vasodilation in mice and humans. Proc Natl Acad Sci U S A. 2006;103(17):6682-6687.