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Laropiprant

Chemical Structure : Laropiprant

CAS No.: 571170-77-9

Laropiprant (MK0524, MK-0524)

货号: PC-45826Not For Human Use, Lab Use Only.

Laropiprant (MK-0524) is a potent and selective prostaglandin D2 (PGD2) receptor (DP1) antagonist with Ki of 0.57 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Laropiprant (MK-0524) is a potent and selective prostaglandin D2 (PGD2) receptor (DP1) antagonist with Ki of 0.57 nM.
Laropiprant shows weaker affinity for TP (Ki=2.95 nM), no significant activity on EP1, EP2, EP3, EP4, FP, and IP.
Laropiprant inhibits the accumulation of cAMP in washed platelets and in plateletrich plasma challenged with PGD with IC50 of 0.09 nM and 4 nM, respectively.
Laropiprant displays an excellent rat pharmacokinetic profile and efficacious in a sheep model of allergic rhinitis.

物理化学性质&存储条件

分子量 435.8963
分子式 C21H19ClFNO4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Cyclopent[b]indole-3-acetic acid, 4-[(4-chlorophenyl)methyl]-7-fluoro-1,2,3,4-tetrahydro-5-(methylsulfonyl)-, (3R)-

参考文献

1. Sturino CF, et al. J Med Chem. 2007 Feb 22;50(4):794-806.

2. Cheng K, et al. Proc Natl Acad Sci U S A. 2006 Apr 25;103(17):6682-7.

3. Philip G, et al. J Allergy Clin Immunol. 2009 Nov;124(5):942-8.e1-9.

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