Taurolithocholic Acid (sodium salt)是一种强效的，可帮助吸收肠道中脂质和甾醇的牛磺酸共轭胆汁酸。
Cas No.:6042-32-6
Sample solution is provided at 25 µL, 10mM.
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Taurolithocholic Acid (sodium salt) is a potent, taurine-conjugated bile acid that facilitates the absorption of lipids and sterols in the intestine[1]. Taurine-conjugated bile acids, compounds formed via amide bonds between bile acids and taurine, play a central role in emulsifying fats, maintaining cholesterol homeostasis, and regulating host metabolism[2]. Taurolithocholic Acid (sodium salt) is commonly used in research on bile acid signaling, cholestasis, and hepatobiliary/pancreatic diseases[3,4].
In vitro, treatment of freshly isolated rat hepatocytes with Taurolithocholic Acid (sodium salt) (5µM) for 5-60min resulted in a sustained and significant activation of PI3K-dependent protein kinase B (PKB/Akt), reaching 194% of the control group's activity at 60min[5]. Treatment of short-term cultured rat hepatocytes with Taurolithocholic Acid (sodium salt) (10µM) for 10min selectively induced the translocation of ε-protein kinase C (ε-PKC) to the cell membrane, increasing its membrane-bound fraction by approximately 47.9%, while showing no significant effect on the distribution of α-, δ-, or ζ-PKC isoforms[6].
In vivo, intravenous administration of Taurolithocholic Acid (sodium salt) (5-100mg/kg) to male Sprague Dawley rats induced dose-dependent cholestasis. The 100mg/kg dose nearly immediately halted bile flow after injection, with gradual recovery observed over 24-30h[7].
References:
[1] XU J, XIE S, CHI S, et al. Protective effects of taurocholic acid on excessive hepatic lipid accumulation via regulation of bile acid metabolism in grouper[J]. Food & Function, 2022, 13(5): 3050-3062.
[2] GUZIOR D V, QUINN R A. Microbial transformations of human bile acids[J]. Microbiome, 2021, 9(1): 140.
[3] DENK G U, MAITZ S, WIMMER R, et al. Conjugation is essential for the anticholestatic effect of NorUrsodeoxycholic acid in taurolithocholic acid–induced cholestasis in rat liver[J]. Hepatology, 2010, 52(5): 1758-1768.
[4] ZHANG Z, GUO X, LIU J, et al. Conjugated bile acids alleviate acute pancreatitis through inhibition of TGR5 and NLRP3 mediated inflammation[J]. Journal of Translational Medicine, 2024, 22(1): 1124.
[5] BEUERS U, DENK G U, SOROKA C J, et al. Taurolithocholic acid exerts cholestatic effects via phosphatidylinositol 3-kinase-dependent mechanisms in perfused rat livers and rat hepatocyte couplets[J]. Journal of Biological Chemistry, 2003, 278(20): 17810-17818.
[6] BEUERS U, PROBST I, SOROKA C, et al. Modulation of protein kinase C by taurolithocholic acid in isolated rat hepatocytes[J]. Hepatology, 1999, 29(2): 477-482.
[7] PRIESTLY B G, CÔTÉ M G, PLAA G L. Biochemical and morphological parameters of taurolithocholate-induced cholestasis[J]. Canadian Journal of Physiology and Pharmacology, 1971, 49(12): 1078-1091.
Taurolithocholic Acid (sodium salt)是一种强效的，可帮助吸收肠道中脂质和甾醇的牛磺酸共轭胆汁酸[1]。牛磺酸共轭胆汁酸是胆汁酸与牛磺酸通过酰胺键结合形成的化合物，在乳化脂肪、维持胆固醇稳态和调节宿主代谢等方面发挥核心作用[2]。Taurolithocholic Acid (sodium salt)通常用于胆汁酸信号转导、胆汁淤积和肝胆/胰腺相关疾病的研究[3,4]。
在体外，Taurolithocholic Acid (sodium salt)（5μM）处理离体培养的大鼠肝细胞5-60min，能持续且显著地激活PI3K依赖的蛋白激酶B（PKB/Akt），在60min时活性达到对照组的194%[5]。Taurolithocholic Acid (sodium salt)（10μM）处理离体短期培养的大鼠肝细胞10min，能选择性诱导ε-蛋白激酶C（ε-PKC）向细胞膜转位，使其膜结合部分增加约47.9%，而对α-、δ-和ζ-PKC亚型的分布无显著影响[6]。
在体内，Taurolithocholic Acid (sodium salt)（5-100mg/kg）经静脉注射给药于雄性Sprague Dawley大鼠，可诱导剂量依赖性胆汁淤积，其中100mg/kg剂量可在注射后几乎立即停止胆汁流动，并在24-30h内逐渐恢复[7]。
| Cell experiment [1]: | |
Cell lines | Hepatocytes (isolated form male Wistar rats) |
Preparation Method | Incubating short-term cultured isolated rat hepatocytes with Taurolithocholic Acid (sodium salt) (10µM) for 10min, followed by homogenization and separation into cytosolic and particulate membrane fractions via ultracentrifugation. The distribution changes of various PKC isoforms were then detected by immunoblotting. Membrane‑bound fractions were quantified by densitometric analysis, and the translocation extent was expressed as the percentage of optical density in the membrane fraction relative to the total (cytosolic + membrane) optical density. |
Reaction Conditions | 10μM; 10min |
Applications | Taurolithocholic Acid (sodium salt) treatment selectively induces ε-PKC translocation to the cell membrane, increasing its membrane-bound portion by approximately 47.9%, while having no significant effect on the distribution of α-, δ-, and ζ-PKC isoforms. |
| Animal experiment [2]: | |
Animal models | Male Sprague Dawley rat |
Preparation Method | Rats were intravenously injected with Taurolithocholic Acid (sodium salt) (5-100mg/kg), and serial bile samples were collected via common bile duct cannulation, with bile flow measured gravimetrically. |
Dosage form | 5, 10, 25, 50, 100mg/kg; i.v. |
Applications | Treatment with Taurolithocholic Acid (sodium salt) can induce dose-dependent cholestasis, with a dose of 100mg/kg causing bile flow to stop almost immediately after injection and gradually recover within 24-30h. |
References: | |
| Cas No. | 6042-32-6 | SDF | |
| 别名 | 牛磺石胆酸钠 | ||
| Canonical SMILES | O=C(NCCS([O-])(=O)=O)CC[C@@H](C)[C@@]1([H])CC[C@@]2([H])[C@]3([H])CC[C@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC[C@@]21C.[Na+] | ||
| 分子式 | C26H44NO5S•Na | 分子量 | 505.7 |
| 溶解度 | DMF: 25 mg/ml,DMSO: 20 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): 1 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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9775 mL | 9.8873 mL | 19.7746 mL |
| 5 mM | 395.5 μL | 1.9775 mL | 3.9549 mL |
| 10 mM | 197.7 μL | 988.7 μL | 1.9775 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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