store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 80 mg/mL (186.69 mM), sonification is recommended.
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
CP-105696 158081-99-3 Immunology/Inflammation LTR CP 105696 CP105696 Pfizer 105696 Inhibitor inhibitor inhibit