Succinobucol (AGI-1067)
(Synonyms: AGI-1067; Probucol monosuccinate) 目录号 : GC31709
A probucol derivative with diverse biological activities
Cas No.:216167-82-7
Sample solution is provided at 25 µL, 10mM.
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Succinobucol is a metabolically stable derivative of probucol with diverse biological activities.1,2,3 It inhibits hydrogen peroxide-induced oxidation of the redox-sensitive dye H2DCF in human pulmonary artery endothelial cells (HPAECs) and U937 cells when used at concentrations of 5 and 10 ?M.1 Succinobucol (0.3-10 ?M) reduces LPS-induced production of IL-6, IL-1β, and TNF-α in peripheral blood mononuclear cells (PBMCs). It suppresses TNF-α-induced vascular cell adhesion molecule 1 (VCAM-1) promoter reporter gene expression in human aortic endothelial cells.2 Succinobucol (50 and 100 mg/kg) lowers plasma LDL levels and increases HDL levels in hypercholesterolemic cynomolgus monkeys.3 It also inhibits the formation of aortic atherosclerotic plaques in ApoE-/- or Ldlr-/- mice.
1.Kunsch, C., Luchoomun, J., Grey, J.Y., et al.Selective inhibition of endothelial and monocyte redox-sensitive genes by AGI-1067: a novel antioxidant and anti-inflammatory agentJ. Pharmacol. Exp. Ther.308(3)820-829(2004) 2.Wasserman, M.A., Sundell, C.L., Kunsch, C., et al.Chemistry and pharmacology of vascular protectants: a novel approach to the treatment of atherosclerosis and coronary artery diseaseAm. J. Cardiol.91(3A)34A-40A(2003) 3.Sundell, C.L., Somers, P.K., Meng, C.Q., et al.AGI-1067: a multifunctional phenolic antioxidant, lipid modulator, anti-inflammatory and antiatherosclerotic agentJ. Pharmacol. Exp. Ther.305(3)1116-1123(2003)
Cell experiment: | The cytotoxicity of Succinobucol is determined in the metastatic 4T1 breast cancer cells. Cells are added to 96-well plates at 6×103 cells/well and cultured overnight. Then, Succinobucol, SCB and the PCD polymer (equivalent concentration to SCB) are respectively added to each well with SCB concentrations ranging from 4 ng/mL to 40 μg/mL. Cells without any treatment are performed as negative control. Thereafter, cells are incubated for further 48 h, and the cell viability is measured by MTT assay method. |
Animal experiment: | Mice are injected with 2×105 4T1-luc cells per mouse to generate the lung metastatic breast cancer model. After the inoculation, mice are divided into three groups (n=4), and respectively treated with saline, SCB solution and Succinobucol (40 mg/kg) by tail injection every three days. At day 12, the formation of lung metastasis is determined by in vivo bioluminescence measurements. Then, mice are autopsied and the lung tissues are removed. In each lung tissue, the visually detected metastatic nodules are counted. The inhibition of lung metastasis is calculated as the average metastatic nodules in Succinobucol or SCB group compared to that in saline group. Moreover, the histological examination is performed by H&E staining to detect the metastatic foci in the lungs. |
References: [1]. Houston SA, et al. An investigation of the antiplatelet effects of succinobucol (AGI-1067). Platelets. 2017 May;28(3):295-300. | |
| Cas No. | 216167-82-7 | SDF | |
| 别名 | AGI-1067; Probucol monosuccinate | ||
| Canonical SMILES | CC(C)(C)C1=CC(SC(C)(C)SC2=CC(C(C)(C)C)=C(OC(CCC(O)=O)=O)C(C(C)(C)C)=C2)=CC(C(C)(C)C)=C1O | ||
| 分子式 | C35H52O5S2 | 分子量 | 616.91 |
| 溶解度 | DMSO : ≥ 100 mg/mL (162.10 mM);Water : < 0.1 mg/mL (insoluble) | 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。 |
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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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.621 mL | 8.1049 mL | 16.2098 mL |
| 5 mM | 0.3242 mL | 1.621 mL | 3.242 mL |
| 10 mM | 0.1621 mL | 0.8105 mL | 1.621 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 |
| 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 | ||||||||||
计算结果:
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet