Home>>Signaling Pathways>> GPCR/G protein>> Leukotriene Receptor>>CP-105696 (Pfizer 105696)

CP-105696 (Pfizer 105696) Sale

(Synonyms: Pfizer 105696) 目录号 : GC32015

CP-105696 (Pfizer 105696)是一种结构新颖、有效并具有选择性的白三烯B4(LTB4)受体拮抗剂,IC50为8.42nM。

CP-105696 (Pfizer 105696) Chemical Structure

Cas No.:158081-99-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,078.00
现货
5mg
¥980.00
现货
10mg
¥1,414.00
现货
25mg
¥2,870.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

Description

CP-105696 (Pfizer 105696) is a structurally novel, effective and selective leukotriene B4 (LTB4) receptor antagonist with an IC50 of 8.42nM[1]. LTB4 is a leukotriene substance related to inflammatory responses, which can induce the formation of reactive oxygen species and the release of enzymes in lysosomes[2]. CP-105696 antagonizes the effects of LTB4 or LTB4 receptor ligands and may inhibit the important inflammatory circuits in the early post-transplantation period[3,4].

In vitro, human neutrophils were treated with CP-105696 (0.3nM), which significantly inhibited the binding of [3H]LTB4 to the high-affinity LTB4 receptor of human neutrophils, with an lC50 value of 8.42±0.26nM. CP-105696 inhibited LTB4 (5nM) -mediated human neutrophil chemotaxis in a non-competitive manner, with an IC50 value of 5.0±2nM[1]. CP-105696 inhibits LTB4-mediated chemotaxis of monkey neutrophils and suppresses the recruitment of neutrophils to the inflammatory site[2].

In vivo, CP-105696 (10, 50, 100mg/kg) was orally administered by gavage in mice that underwent ectopic heart transplantation. After 28 days of treatment, the expression of CD11 anti-anisinin family members (CD11b) in the non-lymphocytic cell population of infiltrating cells in the transplanted heart decreased, reducing the inflammatory response of isolin resistance in immune rejection[3].

References:
[1]Showell HJ, Pettipher ER, Cheng JB, Breslow R, Conklyn MJ, Farrell CA, Hingorani GP, Salter ED, Hackman BC, Wimberly DJ, et al. The in vitro and in vivo pharmacologic activity of the potent and selective leukotriene B4 receptor antagonist CP-105696. J Pharmacol Exp Ther. 1995 Apr;273(1):176-84. PMID: 7714764.
[2]Turner CR, Breslow R, Conklyn MJ, Andresen CJ, Patterson DK, Lopez-Anaya A, Owens B, Lee P, Watson JW, Showell HJ. In vitro and in vivo effects of leukotriene B4 antagonism in a primate model of asthma. J Clin Invest. 1996 Jan 15;97(2):381-7.
[3]Weringer EJ, Perry BD, Sawyer PS, Gilman SC, Showell HJ. Antagonizing leukotriene B4 receptors delays cardiac allograft rejection in mice. Transplantation. 1999 Mar 27;67(6):808-15.
[4]Corry RJ, Winn HJ, Russell PS. Primarily vascularized allografts of hearts in mice. The role of H-2D, H-2K, and non-H-2 antigens in rejection. Transplantation. 1973 Oct;16(4):343-50.

CP-105696 (Pfizer 105696)是一种结构新颖、有效并具有选择性的白三烯B4(LTB4)受体拮抗剂,IC50为8.42nM[1]。LTB4是一种与炎症反应有关的白三烯类物质,够诱导形成活性氧和溶酶体中酶的释放[2]。CP-105696拮抗LTB4或LTB4受体配体的作用,可能抑制移植后早期重要炎症回路[3,4]

在体外,CP-105696(0.3 nM)处理人中性粒细胞,显著抑制[3H]LTB4与人中性粒细胞高亲和力LTB4受体结合,IC50值为8.42±0.26nM。CP-105696以非竞争性方式抑制LTB4(5nM)介导的人中性粒细胞趋化性,IC50值为 5.0±2nM[1]。CP-105696抑制LTB4介导的猴中性粒细胞趋化性,抑制中性粒细胞募集到炎症部位[2]

在体内,CP-105696(10、50、100mg/kg)口服灌胃给药于接受异位心脏移植手术的小鼠,治疗28天后,移植心脏中浸润细胞中的非淋巴细胞群中的CD11抗原样家族成员(CD11b)表达减少,降低免疫排斥中的炎症反应岛素抵抗[3]

实验参考方法

Cell experiment [1]:

Cell lines

Monkey neutrophil cells

Preparation Method

Inhibition of LTB4-mediated chemotaxis of monkey neutrophils by CP105696. LTB4 was used at a fixed concentration of 5nM in the lower chamber, and CP-105696 was present in 0.001, 0.01, 0.1, 1mM concentrations in the upper and lower chambers. Chambers were incubated for 60min at 37℃, and then the filters were removed, processed and counted as described in Methods.

Reaction Conditions

0.001, 0.01, 0.1, 1mM; 60min; 37℃

Applications

CP-105696 inhibits LTB4-mediated chemotaxis of monkey neutrophils and suppresses the recruitment of neutrophils to the inflammatory site.

Animal experiment [2]:

Animal models

C57Bl/6

Preparation Method

CP-105696 was evaluated in (1) a 28-day treatment protocol (50 mg/kg/day), (2) a high-dose (100 mg/kg/day) induction protocol (day 1 to day 3), and (3) a low-dose (10 mg/kg/day) induction protocol (day 1 to day 3). In all study groups, drug was administered orally in a 0.5% methylcellulose vehicle. In parallel studies, treatment of C57Bl/6 recipients bearing B10. BR (H2k) cardiac allografts given FK506 (2 mg/kg/day for 28 days).

Dosage form

10, 50, 100mg/kg; 28 days; i.g.

Applications

CP-105696 reduces the expression of CD11 anti-protoxis family members (CD11b) in the non-lymphocytic cell population of infiltrating cells in the transplanted heart and lowers the inflammatory response in immune rejection.

References:
[1]Turner CR, Breslow R, Conklyn MJ, Andresen CJ, Patterson DK, Lopez-Anaya A, Owens B, Lee P, Watson JW, Showell HJ. In vitro and in vivo effects of leukotriene B4 antagonism in a primate model of asthma. J Clin Invest. 1996 Jan 15;97(2):381-7.
[2]Weringer EJ, Perry BD, Sawyer PS, Gilman SC, Showell HJ. Antagonizing leukotriene B4 receptors delays cardiac allograft rejection in mice. Transplantation. 1999 Mar 27;67(6):808-15.

化学性质

Cas No. 158081-99-3 SDF
别名 Pfizer 105696
Canonical SMILES O=C(C1(C2=CC=C3[C@H](O)[C@@H](CC4=CC=C(C5=CC=CC=C5)C=C4)COC3=C2)CCCC1)O
分子式 C28H28O4 分子量 428.52
溶解度 Soluble in DMSO 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 2.3336 mL 11.6681 mL 23.3361 mL
5 mM 0.4667 mL 2.3336 mL 4.6672 mL
10 mM 0.2334 mL 1.1668 mL 2.3336 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置

产品文档

Quality Control & SDS

View current batch: