CAM-IN-1
目录号 : GC31703CAM-IN-1 是一种有效的选择性 E-selectin 和 ICAM-1 抑制剂,IC50 值分别为 7 和 5 nM。
Cas No.:251994-14-6
Sample solution is provided at 25 µL, 10mM.
CAM-IN-1 is a potent and selective inhibitor of E-selectin and ICAM-1 with IC50 values of 7 and 5 nM, respectively.
CAM-IN-1 shows significant efficacy in a rat rheumatoid arthritis model and in a mouse asthma model. CAM-IN-1 reduces the width of inflamed ankles after the ninth day following treatment, but shows no efficacy in the acute phase. Treatment with CAM-IN-1 (25 mg/kg) for 21 days significantly reduces the ankle inflammation of the arthritis rats. Significant reduction of eosinophils and serum-soluble ICAM-1 (sICAM-1) is observed[1].
[1]. Zhu GD, et al. Selective inhibition of ICAM-1 and E-selectin expression in human endothelial cells. 2. Arylmodifications of 4-(aryloxy)thieno[2,3-c]pyridines with fine-tuning at C-2 carbamides. J Med Chem. 2001 Oct 11;44(21):3469-87.
Animal experiment: | Rats: In a rat rheumatoid arthritis model, 26 all rats are treated with peptidoglycan polysaccharide to elicit the disease to a desired degree. Six rats per group are then treated with ICAM-1-IN-1 or vehicle control twice daily. The ankles of these rats are measured on day 0, 1, 3, 7, 9, 11, 16, 18, and 21 after administration. Histologic analyses of the ankles are performed on the last day of the experiment[1]. |
References: [1]. Zhu GD, et al. Selective inhibition of ICAM-1 and E-selectin expression in human endothelial cells. 2. Arylmodifications of 4-(aryloxy)thieno[2,3-c]pyridines with fine-tuning at C-2 carbamides. J Med Chem. 2001 Oct 11;44(21):3469-87. |
Cas No. | 251994-14-6 | SDF | |
Canonical SMILES | O=C(C(S1)=CC2=C1C=NC=C2OC3=CC=C(Br)C=C3)NC | ||
分子式 | C15H11BrN2O2S | 分子量 | 363.23 |
溶解度 | DMSO : ≥ 135 mg/mL (371.67 mM) | 储存条件 | Store at -20°C |
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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。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.7531 mL | 13.7654 mL | 27.5308 mL |
5 mM | 0.5506 mL | 2.7531 mL | 5.5062 mL |
10 mM | 0.2753 mL | 1.3765 mL | 2.7531 mL |
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 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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