PZ0363
CP-105,696
≥98% (HPLC)
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
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关于此项目
经验公式（希尔记法）:
C28H28O4
化学文摘社编号:
分子量:
428.52
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
assay
≥98% (HPLC)
form
powder
color
white to beige
storage temp.
room temp
SMILES string
OC(C1(CCCC1)C(C=C2)=CC3=C2[C@H](O)[C@@H](CC4=CC=C(C5=CC=CC=C5)C=C4)CO3)=O
InChI key
KMNLXCBYBKHKSK-BKMJKUGQSA-N
Application
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。
Biochem/physiol Actions
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）。
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_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
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| PZ0363-25MG | 04061835502196 |
| PZ0363-5MG | 04061835502202 |