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首页-小分子抑制剂&激动剂-GPCR-Leukotriene Receptor-CP105696
CP105696

Chemical Structure : CP105696

CAS No.: 158081-99-3

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CP105696 (CP-105696)

货号: PC-25787Not For Human Use, Lab Use Only.

CP105696 (CP-105696) is a highly potent, selective leukotriene B4 (LTB4) receptor 1 (BLT1) antagonist, inhibits binding of [3H]LTB4 to whole human neutrophils with IC50 of 5.6 nM, inhibits LTB4 induced chemotaxis of human neutrophils with IC50 of 5.2 nM.

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

生物&药学活性

CP105696 (CP-105696) is a highly potent, selective leukotriene B4 (LTB4) receptor 1 (BLT1) antagonist, inhibits binding of [3H]LTB4 to whole human neutrophils with IC50 of 5.6 nM, inhibits LTB4 induced chemotaxis of human neutrophils with IC50 of 5.2 nM.
CP105696 competitively inhibits LTB4-mediated CD11b upregulation on human neutrophil (pA2 = 8.0).
CP105696 (10 uM) does not inhibit either human neutrophil chemotaxis or CD11b upregulation mediated through alternate (i.e., C5a, IL-8, PAF) G-protein coupled chemotactic factor receptors.
CP105696 inhibits LTB4 (5 nM)-mediated Ca++ mobilization in isolated human monocytes with IC50 of 940 nM.
CP-105696 blocked neutrophil and eosinophil infiltration in cavine dermis mediated by either LTB4 or arachidonic acid with ED50 values of 0.3 +/- 0.1 mg/kg.

物理化学性质&存储条件

分子量 428.53
分子式 C28H28O4
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

1-((3S,4R)-3-([1,1'-Biphenyl]-4-ylmethyl)-4-hydroxychroman-7-yl)cyclopentane-1-carboxylic acid

参考文献

1. Showell HJ, et al. J Pharmacol Exp Ther. 1995 Apr;273(1):176-84.

2. Koch K, et al. J Med Chem. 1994 Sep 30;37(20):3197-9.

3. Griffiths RJ, et al. Proc Natl Acad Sci U S A. 1995 Jan 17;92(2):517-21.

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