Ursodiol
(Synonyms: 熊去氧胆酸; Ursodeoxycholate; Ursodiol; UDCA) 目录号 : GC13363
Ursodiol（UDCA）是一种微生物通过初级胆汁酸鹅去氧胆酸（CDCA）的7α/β 异构化转化而来的次级胆汁酸。Ursodiol可用于多种肝脏疾病和胃肠道疾病的研究。
Cas No.:128-13-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
Cell lines | Hepatoma cells BEL7402 and HepG2 and normal liver cells L-02 |
Preparation Method | Hepatoma cells BEL7402 and HepG2 and normal liver cells L-02 were treated with Ursodiol at concentrations ranging from 0.05mmol/L to 1.0mmol/L, and the cell growth inhibition rate was detected by MTT method at 48 hours, 72 hours and 96 hours. |
Reaction Conditions | 0.05 mmol/L-1.0 mmol/L, 48,72 and 96 h |
Applications | Ursodiol can inhibit the viability of HepG2 and BEL7402 cells. After 48 hours of Ursodiol treatment, the IC50 values of HepG2 and BEL7402 were 0.92 mmol/L and 0.86 mmol/L, respectively. |
| Animal experiment [2]: | |
Animal models | C57BL/6J wildtype mice |
Preparation Method | Five-week-old C57BL/6J WT mice (male and female) were treated with three different doses of Ursodiol (50, 150 and 450 mg/kg) for 21 days, and the mice were weighed daily during the experimental period. |
Dosage form | 50, 150 and 450 mg/kg/day, 21 days, i.g. |
Applications | Compared with the control mice, the mice in the 50 and 450 mg/kg Ursodiol treatment groups continued to lose weight within one week of Ursodiol administration, and there was no significant difference in the body weight of the mice in the 150 mg/kg Ursodiol treatment group. |
References: | |
Ursodiol (UDCA) is a secondary bile acid derived from the 7α/β isomerization of the primary bile acid chenodeoxycholic acid (CDCA) by microorganisms. Ursodiol can be used in the study of various liver diseases and gastrointestinal diseases. Ursodiol has cytoprotective, anti-apoptotic, membrane-stabilizing, antioxidant and immunomodulatory effects[1-3].
Ursodiol can inhibit the viability of HepG2 and BEL7402 cells with IC50 of 0.92 mmol/L and 0.86 mmol/L, respectively, but Ursodiol has no effect on the viability of normal hepatocytes L-02. After Ursodiol (1.0 mmol/L) treatment, the apoptosis rate of HepG2 and BEL7402 cells was significantly increased in a concentration-dependent manner, whereas the apoptosis rate of L-02 cells did not change significantly.Ursodiol inhibits Bcl-2 expression and promotes Bax expression [2].
Mice treated with low and high doses (50 and 450 mg/kg/day) of Ursodiol showed significant weight loss, whereas 150 mg/kg/day had no significant effect on mouse body weight. After 21 days of ursodiol treatment, the microbial community structure and bile acid pool in the ileum and cecum contents and feces of mice were significantly changed compared with those before treatment. Ursodeoxycholic acid (UDCA), Tauroursodeoxycholic acid (TUDCA), Glycoursodeoxycholic acid (GUDCA) and Lithocholic acid (LCA) levels were significantly elevated in the ileum of mice treated with Ursodiol 450 mg/kg[1]. Ursodiol treatment at 416 mg/kg reduces SARS-CoV-2 transmission in a Syrian golden hamster SARS-CoV-2 infection model[4].
References:
[1]Winston JA, Rivera A, Cai J, Patterson AD, Theriot CM. Secondary bile acid ursodeoxycholic acid alters weight, the gut microbiota, and the bile acid pool in conventional mice. PLoS One. 2021 Feb 18;16(2):e0246161.
[2] Liu H, Qin CY, Han GQ, Xu HW, Meng M, Yang Z. Mechanism of apoptotic effects induced selectively by ursodeoxycholic acid on human hepatoma cell lines. World J Gastroenterol. 2007 Mar 21;13(11):1652-8.
[3] Kumar D, Tandon RK. Use of ursodeoxycholic acid in liver diseases. J Gastroenterol Hepatol. 2001 Jan;16(1):3-14.
[4] Brevini T, Maes M, Webb G J, et al. FXR inhibition may protect from SARS-CoV-2 infection by reducing ACE2[J]. Nature, 2023, 615(7950): 134-142.
Ursodiol（UDCA）是一种微生物通过初级胆汁酸鹅去氧胆酸（CDCA）的7α/β异构化转化而来的次级胆汁酸。Ursodiol可用于多种肝脏疾病和胃肠道疾病的研究。Ursodiol具有细胞保护、抗凋亡、膜稳定、抗氧化和免疫调节作用[1-3]。
Ursodiol可抑制HepG2和BEL7402细胞的活力，IC50分别为0.92 mmol/L和0.86 mmol/L，但Ursodiol对正常肝细胞L-02的活力没有影响。Ursodiol（1.0 mmol/L）处理后，HepG2和BEL7402细胞的凋亡率显著增加，且呈浓度依赖性，而L-02细胞凋亡率没有明显变化。Ursodiol可抑制Bcl-2表达，促进Bax表达[2]。
使用低剂量和高剂量（50和450 mg/kg/天）的Ursodiol治疗的小鼠体重明显减轻，而150 mg/kg对小鼠体重没有显著影响。与治疗前相比，Ursodiol治疗21天后，小鼠回肠和盲肠内容物以及粪便中微生物群落结构和胆汁酸库发生了明显变化。Ursodiol 450mg/kg处理时，小鼠回肠内熊去氧胆酸（UDCA）、牛黄熊去氧胆酸（TUDCA）、甘氨熊脱氧胆酸（GUDCA）和石胆酸（LCA）含量显著升高[1]。在叙利亚金仓鼠SARS-CoV-2感染模型中，416 mg/kg的Ursodiol治疗可减少SARS-CoV-2传播[4]。
| Cas No. | 128-13-2 | SDF | |
| 别名 | 熊去氧胆酸; Ursodeoxycholate; Ursodiol; UDCA | ||
| 化学名 | (4R)-4-[(3R,5S,7S,8R,9S,10S,13R,14S,17R)-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoic acid | ||
| Canonical SMILES | CC(CCC(=O)O)C1CCC2C1(CCC3C2C(CC4C3(CCC(C4)O)C)O)C | ||
| 分子式 | C24H40O4 | 分子量 | 392.57 |
| 溶解度 | ≥ 16mg/mL in DMSO | 储存条件 | Store at 4°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 | 2.5473 mL | 12.7366 mL | 25.4732 mL |
| 5 mM | 0.5095 mL | 2.5473 mL | 5.0946 mL |
| 10 mM | 0.2547 mL | 1.2737 mL | 2.5473 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。
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