Cholesteryl Hemisuccinate
(Synonyms: 胆固醇琥珀酸单酯) 目录号 : GC43258
Cholesteryl Hemisuccinate是一种酸性胆固醇酯，具有肝保护和抗癌活性。
Cas No.:1510-21-0
Sample solution is provided at 25 µL, 10mM.
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Cholesteryl Hemisuccinate is an acidic cholesterol ester with hepatoprotective and anticancer activities[1, 2]. Cholesteryl Hemisuccinate inhibits DNA polymerase and DNA topoisomerase and promotes DNA replication and repair[3]. Cholesteryl Hemisuccinate is a detergent widely used in protein crystallography, protein biochemistry research and pharmacology[4]. Cholesteryl Hemisuccinate can inhibit the attachment and spreading of epithelial cells[5].
In vivo, Cholesteryl Hemisuccinate (100mg/kg) pre-treated ICR mice treated with acetaminophen (AAP) by intraperitoneal injection inhibited AAP-induced liver injury and suppressed hepatocyte necrosis and apoptosis[6].
References:
[1] Fariss M W, Fortuna M B, Everett C K, et al. The selective antiproliferative effects of α-tocopheryl hemisuccinate and cholesteryl hemisuccinate on murine leukemia cells result from the action of the intact compounds[J]. Cancer Research, 1994, 54(13): 3346-3351.
[2] Shah H, Madni A, Khan M M, et al. pH-responsive liposomes of dioleoyl phosphatidylethanolamine and cholesteryl hemisuccinate for the enhanced anticancer efficacy of cisplatin[J]. Pharmaceutics, 2022, 14(1): 129.
[3] Varshosaz J, Taymouri S, Hassanzadeh F, et al. Folated Synperonic‐Cholesteryl Hemisuccinate Polymeric Micelles for the Targeted Delivery of Docetaxel in Melanoma[J]. BioMed research international, 2015, 2015(1): 746093.
[4] Kulig W, Jurkiewicz P, Olżyńska A, et al. Experimental determination and computational interpretation of biophysical properties of lipid bilayers enriched by cholesteryl hemisuccinate[J]. Biochimica et Biophysica Acta (BBA)-Biomembranes, 2015, 1848(2): 422-432.
[5] Sauk J J, Krumwiede M, Cooking‐Johnson D, et al. Alterations in lipid fluidity induced by cholesterol and cholesterol hemisuccinate modulate the organization of microtubule skeletons in epithelial cells[J]. Journal of Oral Pathology & Medicine, 1987, 16(2): 69-74.
[6] Ray S D, Mumaw V R, Raje R R, et al. Protection of acetaminophen-induced hepatocellular apoptosis and necrosis by cholesteryl hemisuccinate[J]. Journal of Pharmacology and Experimental Therapeutics, 1996, 279: 1470-1483.
Cholesteryl Hemisuccinate是一种酸性胆固醇酯，具有肝保护和抗癌活性[1, 2]。Cholesteryl Hemisuccinate 抑制DNA聚合酶和DNA拓扑异构酶，促进DNA复制和修复[3]。Cholesteryl Hemisuccinate是一种去垢剂，广泛应用于蛋白质晶体学、蛋白质生化研究和药理学[4]。Cholesteryl Hemisuccinate能够抑制上皮细胞的附着和扩散[5]。
在体内，Cholesteryl Hemisuccinate（100mg/kg）通过腹腔注射预处理接受乙酰氨基酚（AAP）治疗的ICR小鼠，抑制了AAP诱导的肝损伤，抑制了肝细胞坏死和凋亡[6]。
| Animal experiment [1]: | |
Animal models | ICR mice |
Preparation Method | Acetaminophen (AAP) and Cholesteryl Hemisuccinate both were dissolved in normasaline and administered i.p. The Cholesteryl Hemisuccinate solution was vigorously sonicated forming a uniform suspension and pH adjusted to 7.4. Animals were administered Cholesteryl Hemisuccinate (100mg/kg, i.p.) and were returned to a normal diet for 12h. Nextanimals were fasted for 12h and received AAP exposure. 2h after AAP administration the animals were given free access to food and water. 24h after AAP exposure, animals were killedand tissues (blood and liver)were obtained for biochemical andmorphological analyses. |
Dosage form | 100mg/kg; i.p. |
Applications | Cholesteryl Hemisuccinate pretreatment inhibited AAP-induced liver injury and suppressed hepatocyte necrosis and apoptosis. |
References: [1]Ray S D, Mumaw V R, Raje R R, et al. Protection of acetaminophen-induced hepatocellular apoptosis and necrosis by cholesteryl hemisuccinate[J]. Journal of Pharmacology and Experimental Therapeutics, 1996, 279: 1470-1483. | |
| Cas No. | 1510-21-0 | SDF | |
| 别名 | 胆固醇琥珀酸单酯 | ||
| Canonical SMILES | C[C@]12C(C[C@@H](OC(CCC(O)=O)=O)CC2)=CC[C@]3([H])[C@]1([H])CC[C@@]4(C)[C@@]3([H])CC[C@@]4([C@@H](CCCC(C)C)C)[H] | ||
| 分子式 | C31H50O4 | 分子量 | 486.7 |
| 溶解度 | Chloroform: 10 mg/ml | 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 | 2.0547 mL | 10.2733 mL | 20.5465 mL |
| 5 mM | 0.4109 mL | 2.0547 mL | 4.1093 mL |
| 10 mM | 0.2055 mL | 1.0273 mL | 2.0547 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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet