所有图片(1)
别名:
(+)-1-(3S,4R)- [3-（4-苯基苄基）-4-羟基色烷-7-基] 环戊烷羧酸, 1-[(3S,4R)-3-([1,1′-联苯基 ]-4-基甲基）-3,4-二氢-4-羟基-2H-1-苯并吡喃-7-基 ]-环戊烷羧酸, CP-105696, CP105696
经验公式（希尔记法）:
C28H28O4
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检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
储存温度
room temp
SMILES字符串
OC(C1(CCCC1)C(C=C2)=CC3=C2[C@H](O)[C@@H](CC4=CC=C(C5=CC=CC=C5)C=C4)CO3)=O
应用
CP-105,696已作为白三烯B4受体(LTB4R)拮抗剂，用于研究LTB4通路在过敏性钙化三醇(MC903)+模型变应原卵清蛋白(OVA)致敏小鼠特应性皮炎(AD)样疾病急性瘙痒发作机制中的影响。
生化/生理作用
CP-105,696是一种具有口服活性的有效选择性白三烯 B4 受体 (LTB4R) 拮抗剂（结合人中性粒细胞时，对[3H]LTB4的 IC50 = 5.6 nM；结合豚鼠脾或小鼠膜时，分别为IC50 = 9.7 nM & 30.3 nM），分别以LTB4非竞争性和竞争性方式靶向 LTB4R高亲和力和低亲和力结合位点。CP-105,696可抑制5 nM LTB4诱导的人中性粒细胞趋化性和 CDllb 上调（IC50分别为5.2 nM 和 430 nM），同时不抑制环加氧酶活性或影响C5a、PAF、IL-8诱导的趋化性。口服给药对皮内LTB4（100 ng/小鼠）有效，但对小鼠和豚鼠体内的IL-1、注射诱导中性粒细胞积聚（ED50分别为4.2 和 0.26 mgkg）无效。CP-105,696的体内疗效也在其他动物模型中得到证实，包括胶原诱导性关节炎（CIA；小鼠体内0.3-10 mg/kg）、过敏性脑脊髓炎（ED50= 8.6 mg/kg；小鼠）和哮喘（10- 30 mg/kg；灵长类动物）。
警示用语：
Warning
危险声明
危险分类
Acute Tox. 4 Oral
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
(+)-1-(3S,4R)-[3-(4-phenylbenzyl)-4-hydroxychroman-7-yl]cyclopentane carboxylic acid, a highly potent, selective leukotriene B4 antagonist with oral activity in the murine collagen-induced arthritis model.
K Koch et al.
Journal of medicinal chemistry, 37(20), 3197-3199 (1994-09-30)
R J Griffiths et al.
Proceedings of the National Academy of Sciences of the United States of America, 92(2), 517-521 (1995-01-17)
Leukotriene B4 (LTB4) is a product of the 5-lipoxygenase pathway of arachidonic acid metabolism. LTB4 is a potent chemotactic factor for neutrophils and has been postulated to play an important role in a variety of pathological conditions including rheumatoid arthritis
C R Turner et al.
The Journal of clinical investigation, 97(2), 381-387 (1996-01-15)
To test the hypothesis that leukotriene (LT) B4 antagonists may be clinically useful in the treatment of asthma, CP-105,696 was evaluated in vitro, using chemotaxis and flow cytometry assays, and in vivo, using a primate asthma model. CP-105,696 inhibited LTB4-mediated
Fang Wang et al.
Cell, 184(2), 422-440 (2021-01-16)
Itch is an evolutionarily conserved sensation that facilitates expulsion of pathogens and noxious stimuli from the skin. However, in organ failure, cancer, and chronic inflammatory disorders such as atopic dermatitis (AD), itch becomes chronic, intractable, and debilitating. In addition to
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