CP-105696 Pfizer 105696|cas:158081-99-3|西域试剂

CP-105696 Pfizer 105696,99.66%

产品编号：Bellancom-19193| CAS NO：158081-99-3| 分子式：C₂₈H₂₈O₄| 分子量：428.52

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货号	价格	库存与货期
Bellancom-19193	￥1600.00	杭州北京（现货）
Bellancom-19193	￥2600.00	杭州北京（现货）
Bellancom-19193	￥5200.00	杭州北京（现货）

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CP-105696 Pfizer 105696

产品介绍

CP-105696 是一个有效的、白三烯 B₄ (LTB₄) 受体的选择性拮抗剂，其 IC₅₀ 值为 8.42 nM。

生物活性

CP-105696 is a potent and selective Leukotriene B₄ Receptor antagonist, with an IC₅₀ of 8.42 nM.

体外研究

CP-105696 is a structurally novel, selective and potent LTB₄ receptor antagonist. In vitro, CP-105696 inhibits [³H]LTB₄ (0.3 nM) binding to high-affinity LTB₄ receptors on human neutrophils with an lC₅₀ 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. CP-105696 inhibits human neutrophil chemotaxis mediated by LTB₄ (5 nM) in a noncompetitive manner 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, and inhibition of LTB₄-mediated CD11b upregulation on human neutrophils is competitively inhibited by CP-105696 (pA₂=8.03±0.19). CP-105696 at 10 μM does not inhibit either human neutrophil chemotaxis or CD11b upregulation mediated through alternate (i.e., C5a, lL-8, PAF) G-protein coupled chemotactic factor receptors. In isolated human monocytes, LTB₄ (5 nM)-mediated Ca²⁺ mobilization is inhibited by CP-105696 with an lC₅₀ value of 940±70 nM.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

At a dose of 50 mg/kg/day (28 days), B10.BR (H2k) allografts transplanted into C57Bl/6 (H2b) recipients are significantly protected, as reflected by the mean survival time versus control grafts (27±20 days [n=10] vs. 12±6 days [n=14]; P=0.0146). Using 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), but CP-105696 at 10 mg/kg/day does not (18±16 days [n=8]; P=0.1433). Syngeneic grafts survive indefinitely (n=11). Immunohistological evaluation of allografts at rejection reveals a mononuclear cell infiltrate composed primarily 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 demonstrat a selective reduction in β2-integrin (Mac-1) expression on monocytes/macrophages, as demonstrated by CD11b staining density compared with allograft controls.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (233.36 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	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

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.83 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.83 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.83 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。