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CP-105696

CP-105696

产品编号 T15002   CAS 158081-99-3
别名: Pfizer 105696

CP-105696 是一种具有强效性和选择性白三烯 B4 (LTB4) 受体拮抗剂,可用于研究异体移植物排斥反应。

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CP-105696 Chemical Structure
CP-105696, CAS 158081-99-3
规格 价格/CNY 货期 数量
2 mg ¥ 789 现货
5 mg ¥ 1,330 现货
10 mg ¥ 1,980 现货
25 mg ¥ 3,980 现货
1 mL * 10 mM (in DMSO) ¥ 1,460 现货
产品目录号及名称: CP-105696 (T15002)
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纯度: 99.78%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 CP-105696 is a potent and selective leukotriene B4 (LTB4) receptor antagonist for the study of allograft rejection.
靶点活性 LTB4:8.42±0.26 nM
体外活性 CP-105696 is a structurally novel, selective, and potent LTB4 receptor antagonist. In vitro, it inhibits [3H]LTB4 (0.3 nM) binding to high-affinity LTB4 receptors on human neutrophils with an IC50 value of 8.42±0.26 nM. Scatchard analyses of [3H]LTB4 binding to these high-affinity receptors indicate that CP-105696 acts as a noncompetitive antagonist.In a noncompetitive manner, CP-105696 inhibits human neutrophil chemotaxis mediated by LTB4 (5 nM) with an IC50 value of 5.0±2.0 nM. Scatchard analyses of [3H]LTB4 binding to low-affinity receptors on neutrophils indicate that CP-105696 acts as a competitive antagonist at this receptor. Furthermore, CP-105696 competitively inhibits LTB4-mediated CD11b upregulation on human neutrophils (pA2=8.03±0.19).At 10 μM, CP-105696 does not inhibit either human neutrophil chemotaxis or CD11b upregulation mediated through alternate G-protein coupled chemotactic factor receptors (i.e., C5a, IL-8, PAF). In isolated human monocytes, CP-105696 inhibits LTB4 (5 nM)-mediated Ca2+ mobilization with an IC50 value of 940±70 nM[2].
体内活性 At a dose of 50 mg/kg/day (for 28 days), B10.BR (H2k) allografts transplanted into C57Bl/6 (H2b) recipients show significant protection, as evidenced by the mean survival time compared to control grafts (27±20 days [n=10] vs. 12±6 days [n=14]; P=0.0146). Utilizing an induction protocol (day -1 to day 3), CP-105696 at 100 mg/kg/day significantly prolongs allograft survival (33±23 days [n=9]; P=0.0026), while CP-105696 at 10 mg/kg/day does not (18±16 days [n=8]; P=0.1433). Syngeneic grafts exhibit indefinite survival (n=11).Immunohistological evaluation of allografts at rejection reveals a mononuclear cell infiltrate primarily composed of CD3+ and CD11b+ (Mac-1+) cells, which are infrequent in syngeneic grafts. Allografts from mice treated with CP-105696 at 50 or 100 mg/kg/day demonstrate a selective reduction in β2-integrin (Mac-1) expression on monocytes/macrophages, as indicated by CD11b staining density compared with allograft controls[1].
别名 Pfizer 105696
分子量 428.52
分子式 C28H28O4
CAS No. 158081-99-3

存储

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 80 mg/mL (186.69 mM), sonification is recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3336 mL 11.6681 mL 23.3361 mL 58.3403 mL
5 mM 0.4667 mL 2.3336 mL 4.6672 mL 11.6681 mL
10 mM 0.2334 mL 1.1668 mL 2.3336 mL 5.834 mL
20 mM 0.1167 mL 0.5834 mL 1.1668 mL 2.917 mL
50 mM 0.0467 mL 0.2334 mL 0.4667 mL 1.1668 mL
100 mM 0.0233 mL 0.1167 mL 0.2334 mL 0.5834 mL

计算器

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稀释计算器
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分子量计算器
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参考文献

1. Weringer EJ, et al. Antagonizing leukotriene B4 receptors delays cardiac allograft rejection in mice. Transplantation. 1999 Mar 27;67(6):808-15. 2. Showell HJ, 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.
BIRM 271 3-(4-Hydroxyphenyl)-1-propanol Ticolubant hnps-PLA Inhibitor Tebufelone Etalocib Montelukast trans-Hinokiresinol

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
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g
给药体积
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第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

CP-105696 158081-99-3 Immunology/Inflammation LTR CP 105696 CP105696 Pfizer 105696 Inhibitor inhibitor inhibit

 

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