Sodium Tauroursodeoxycholate (TUDC)
(Synonyms: 牛磺熊去氧胆酸钠; Tauroursodeoxycholic acid sodium; TUDCA sodium; UR 906 sodium) 目录号 : GC17425Tauroursodeoxycholate (Tauroursodeoxycholic acid; TUDCA) sodium 是一种内质网 (ER) 应激抑制剂。 Tauroursodeoxycholate 显着降低凋亡分子的表达,例如 caspase-3 和 caspase-12。 Tauroursodeoxycholate 也抑制 ERK。
Cas No.:35807-85-3
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: |
Cell viability and proliferation are measured using Ez-Cytox. VSMCs (5×103 cells) are seeded onto 96-well plates in Smooth Muscle Cell Growth Medium 2 (SMCGM2) and cultured. After serum starvation, Tauroursodeoxycholate (0, 50, 100, and 200 μM) is added to the hVSMCs, with or without 1,2-bis(o-aminophenoxy) ethane-N,N,N′,N′-tetraacetic acid tetra(acetoxymethyl) ester (BAPTA, 10 μM) and 7-hydroxystaurosporine (H7, 10 μM) and cultured for 24 h. To assess the effect of Tauroursodeoxycholate on the PDGF-stimulated hVSMC proliferation, hVSMCs are seeded onto 96-well plates and cultured. After serum starvation, Tauroursodeoxycholate (0, 50, 100, and 200 μM) is added to the hVSMCs, with or without PDGF-BB (50 ng/mL) and cultured. After addition of 10 μL of Ez-Cytox into each well, cell viability is evaluated by measuring the optical density at 450 nm[1]. |
Animal experiment: |
Rats[1]Sprague-Dawley rats are anaesthetized with a combined anaesthetic (Ketamine, 70 mg/kg; Xylazine, 7 mg/kg ip). Tauroursodeoxycholate is administered orally once a day, in different concentrations (i.e. vehicle, 10, 50, and 100 mg/kg) for 2 weeks. The carotid arteries are fixed by perfusion with 4% formaldehyde, then the tissues are embedded in paraffin, and sections (8 μm) are stained with H&E[1]. Mice[2]Thirty ApoE-/- C57BL/6 male mice aged 8 weeks are randomly divided into three groups (n=10 in each group): (i) sham operated and injected with physiologic (0.9%) saline as vehicle (normal: group); (ii) mini-osmotic pumps are implanted subcutaneously into the right flank of ApoE-/- mice to release Ang II (1000 ng/kg/min) over the course of 28 days (AAA model group); (iii) AAA model mice treated with Tauroursodeoxycholate daily for 4 weeks at a dosage of 0.5 g/kg/day in drinking water (Tauroursodeoxycholate group). Mice are sacrificed after 28 days of Ang II infusion[2]. |
References: [1]. 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. |
Sodium tauroursodeoxycholate (TUDC) shows therapeutic effect on cholestasis [1, 2]. In human erythrocytes, it inhibited 2’,7’-bis-(carboxypropyl)-5(6)-carboxyfluorescein (BCPCF) efflux induced by bile salts with an IC50 value of 560 µM [3].
Cholestasis is the syndrome resulted from the impairment of the formation of bile, a vital function [4].
cVA-of-CLF means the canalicular vacuolar accumulation of cholyllysylfluorescein [1]. cVA of CLF is a parameter to indicate overall biliary secretion [5]. Incubation with 17βEG dose-dependently decreased the cVA-of-CLF in cells. 17βEG at a concentration of 50 µM decreased cVA-of-CLF by 40%. The simultaneous incubation with TUDC and 17βEG improved the decreased cVA by 24%. The simultaneous incubation with SAMe and 17βEG improved the decreased cVA by 18%. The simultaneous incubation with TUDC, SAMe and 17βEG improved the decreased cVA by 28%. But the effect of TUDC + SAMe was not significantly greater than the effect of either protectant alone [1].
In rats, intrahepatic cholestasis was induced by the administration of phalloidin at an i.p. dose of 500 µg/kg for 7 days. In these treated rats, bile flow was decreased, and activities of glutamic pyruvic transaminase, leucine aminopeptidase, serum alkaline phosphatase, and concentrations of bile acid, phospholipid and cholesterol were increased. But these effects were significantly suppressed by tauroursodeoxycholate. In these rats, excretion rates of biliary cholesterol and phospholipid were significantly improved by tauroursodeoxycholate [2].
References:
[1]. Milkiewicz P, Roma MG, Cardenas R, et al. Effect of tauroursodeoxycholate and S-adenosyl-l-methionine on 17β-estradiol glucuronide-induced cholestasis. Journal of hepatology, 2001, 34(2): 184-191.
[2]. Ishizaki K, Kinbara S, Hirabayashi N, et al. Effect of sodium tauroursodeoxycholate on phalloidin-induced cholestasis in rats. European journal of pharmacology, 2001, 421(1): 55-60.
[3]. Mrowczynska L, Bobrowska-Hgerstrand M, Wrobel A, et al. Inhibition of MRP1-mediated efflux in human erythrocytes by mono-anionic bile salts. Anticancer research, 2005, 25(5): 3173-3178.
[4]. Trauner M, Meier PJ, Boyer JL. Molecular pathogenesis of cholestasis. New England Journal of Medicine, 1998, 339(17): 1217-1227.
[5]. Milkiewicz P, Roma MG, Elias E, et al. Hepatoprotection with tauroursodeoxycholate and β muricholate against taurolithocholate induced cholestasis: involvement of signal transduction pathways. Gut, 2002, 51(1): 113-119.
Cas No. | 35807-85-3 | SDF | |
别名 | 牛磺熊去氧胆酸钠; Tauroursodeoxycholic acid sodium; TUDCA sodium; UR 906 sodium | ||
化学名 | sodium (R,Z)-4-((3R,5S,7S,8R,9S,10S,13R,14S,17R)-3,7-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-N-(2-sulfoethyl)pentanimidate | ||
Canonical SMILES | C[C@]([C@@]1([H])CC[C@@]2([H])[C@@]([C@](O)([H])C[C@]3([H])C[C@@](O)([H])CC[C@@]34C)([H])[C@]4([H])CC[C@]12C)([H])CC/C([O-])=N/CCS(O)(=O)=O.[Na+] | ||
分子式 | C26H44NNaO6S | 分子量 | 521.69 |
溶解度 | ≥ 26.1mg/mL in DMSO | 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。 |
||
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 | 1.9168 mL | 9.5842 mL | 19.1685 mL |
5 mM | 0.3834 mL | 1.9168 mL | 3.8337 mL |
10 mM | 0.1917 mL | 0.9584 mL | 1.9168 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。