Tauroursodeoxycholate (TUDCA)
(Synonyms: 牛磺熊去氧胆酸; Tauroursodeoxycholic acid; TUDCA; UR 906) 目录号 : GC34181
牛磺酸脱氧胆酸盐(TUDCA)是包括肝细胞在内的多种细胞的细胞保护剂,也是癌症细胞凋亡的诱导剂。
Cas No.:14605-22-2
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Tauroursodeoxycholate (TUDCA) is a cytoprotective agent in a variety of cells including hepatocytes as well as an inducer of apoptosis in cancer cells[1]. Tauroursodeoxycholate, as an endoplasmic reticulum (ER) stress inhibitor, is effective in protecting the hepatocytes and restoring glucose homeostasis by reducing the endoplasmic reticulum stress[2].
In vitro, 200 µM TUDCA suppressed viability of hVSMCs (vascular smooth muscle cells) by inhibition of ERK (extracellular signal-regulated kinase) phosphorylation, through induction of MKP-1 (MAPK phosphatase-1) via PKCα (protein kinase Cα). And TUDCA inhibited both the proliferation and migration of PDGF-stimulated hVSMCs[1]. In vitro, 25 µM Tauroursodeoxycholate (TUDC) increases plasma membrane multidrug resistance-associated protein 2 (MRP2). And TUDC and cAMP increase Rab11 activity[3].
In vivo, TUDCA prevents the MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine)-dependent decrease of dopaminergic fibers and ATP levels, mitochondrial dysfunction and neuroinflammation. TUDCA administration (50 mg/kg), the mice also displayed reduction in foot dragging and an overall improvement in gait[4]. Mice were treated with TUDCA 0.5 mg/g every 3 days, for a total of 7 injections, which showed an increase in neuromuscular junction innervation in the mutated mice[5]. TUDCA treatment (100 mg, 3 times/day) also reduces neurological impairment in rats with acute cerebral infarction[6].
Kim SY, et al. Tauroursodeoxycholate (TUDCA) inhibits neointimal hyperplasia by suppression of ERK via PKCα-mediated MKP-1 induction. Cardiovasc Res. 2011 Nov 1;92(2):307-16.
Kim SY, et al. Tauroursodeoxycholate (TUDCA) inhibits neointimal hyperplasia by suppression of ERK via PKCα-mediated MKP-1 induction. Cardiovasc Res. 2011 Nov 1;92(2):307-16.
Park SW, et al. Rab11, but not Rab4, facilitates cyclic AMP- and tauroursodeoxycholate-induced MRP2 translocation to the plasma membrane. Am J Physiol Gastrointest Liver Physiol. 2014 Oct 15;307(8):G863-70.
[3] Rosa AI, et al. Tauroursodeoxycholic acid improves motor symptoms in a mouse model of Parkinson's disease. Mol Neurobiol. 2018;55(12):9139-9155.
[4] Thams S, et al. A stem cell-based screening platform identifies compounds that desensitize motor neurons to endoplasmic reticulum stress. Mol Ther. 2019;27(1):87-101.
[5] Bian KY, et al. DCA can improve the ACI-induced neurological impairment through negative regulation of Nrf2 signaling pathway. Eur Rev Med Pharmacol Sci. 2019;23(1):343-351.
References:
牛磺酸脱氧胆酸盐(TUDCA)是包括肝细胞在内的多种细胞的细胞保护剂,也是癌症细胞凋亡的诱导剂[1]。牛磺酸脱氧胆酸盐作为一种内质网应激抑制剂,通过减少内质网应激,有效地保护肝细胞和恢复葡萄糖稳态[2]。
在体外,200µM TUDCA通过抑制ERK(细胞外信号调节激酶)磷酸化,通过PKCα(蛋白激酶Cα)诱导MKP-1(MAPK磷酸酶-1),抑制hVSMCs(血管平滑肌细胞)的活力。TUDCA同时抑制PDGF刺激的hVSMCs的增殖和迁移[1]。在体外,25µM牛磺酸脱氧胆酸盐(TUDC)可增加质膜多药耐药相关蛋白2(MRP2)。TUDC和cAMP可提高Rab11活性[3]。
在体内,TUDCA可防止MPTP(1-甲基-4-苯基-1,2,3,6-四氢吡啶)依赖性多巴胺能纤维和ATP水平的降低、线粒体功能障碍和神经炎症。给予TUDCA(50 mg/kg)后,小鼠的拖脚能力也有所减少,步态也有所改善[4]。每3天用TUDCA 0.5 mg/g治疗小鼠,共注射7次,这表明突变小鼠的神经肌肉接头神经支配增加[5]。TUDCA治疗(100 mg,3次/天)也可减少急性脑梗死大鼠的神经损伤[6]。
| Cell experiment [1]: | |
|
Cell lines |
Hepatocytes and HuH‐NTCP cells |
|
Preparation Method |
Hepatocytes and HuH‐NTCP cells were treated with DMSO (Con), 100 µmol/L CPT‐cAMP (cAMP) for 15 min, 10 µmol/L TLC for 25 min, 100 µmol/L CPT‐cAMP + 10 µmol/L TLC for 25 min, or 25 µmol/L TUDC for 15 min or 10 µmol/L TLC for 25 min or 25 µmol/L TUDC + 10 µmol/L TLC for 25 min. |
|
Reaction Conditions |
25 µmol/L; 25 min |
|
Applications |
Cyclic AMP and TUDC inhibit TLC‐induced increases in plasma membrane PKC ε in rat hepatocytes. Cyclic AMP and TUDC inhibit TLC‐induced increases in plasma membrane PKC ε in HuH‐NTCP cells. |
| Animal experiment [2]: | |
|
Animal models |
TNBS(2,4,6-trinitrobenzene sulfonic acid)-induced ulcerative colitis in mice |
|
Preparation Method |
After the induction of colitis for 24h, the mice were administrated orally with tauroursodeoxycholate (20, 40 and 60mg/kg) and sulfasalazine (500mg/kg) by gavage for 7 consecutive days. The inhibition effects were evaluated by the body of weight change, survival rate, macroscopical and histological evaluations. |
|
Dosage form |
20, 40 and 60mg/kg; p.o. |
|
Applications |
Treatment with different doses of tauroursodeoxycholate (20, 40 and 60mg/kg) significantly improved the body weight change, decreased the macroscopic and histopathological scores. Compared with the model group, the accumulation of MPO activity, the colonic tissue levels of IL-1β, IFN-γ and TNF-α were significantly reduced in the tauroursodeoxycholate treated groups. Moreover, tauroursodeoxycholate assuaged the symptoms of colitis. |
|
References: [1] Park SW, et al. Mechanism of inhibition of taurolithocholate-induced retrieval of plasma membrane MRP2 by cyclic AMP and tauroursodeoxycholate. Physiol Rep. 2017 Dec;5(23):e13529. | |
| Cas No. | 14605-22-2 | SDF | |
| 别名 | 牛磺熊去氧胆酸; Tauroursodeoxycholic acid; TUDCA; UR 906 | ||
| Canonical SMILES | C[C@H](CCC(NCCS(=O)(O)=O)=O)[C@H]1CC[C@@]2([H])[C@]3([H])[C@@H](O)C[C@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC[C@]12C | ||
| 分子式 | C26H45NO6S | 分子量 | 499.7 |
| 溶解度 | Water:12.5mg/mL(25.02 mM) | 储存条件 | Store at RT |
| 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。 |
||
| 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 | 2.0012 mL | 10.006 mL | 20.012 mL |
| 5 mM | 0.4002 mL | 2.0012 mL | 4.0024 mL |
| 10 mM | 0.2001 mL | 1.0006 mL | 2.0012 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet