Tauro-β-muricholic Acid (sodium salt)
(Synonyms: 牛磺-Α-鼠胆酸,Tauro-β-muricholate； TβMCA) 目录号 : GC45000Tauro-β-muricholic Acid (sodium salt)是一种可逆的竞争性法尼基X受体（FXR）拮抗剂（IC50 = 40μM)。
Cas No.:145022-92-0
Sample solution is provided at 25 µL, 10mM.
Tauro-β-muricholic Acid (sodium salt) is a reversible, competitive farnesyl X receptor (FXR) antagonist (IC50 = 40μM) [1]. Tauro-β-muricholic Acid competitively inhibits FXR activation, thereby interfering with the FXR-SHP and FXR-FGF15 pathways, enhancing bile acid synthesis and regulating related metabolic signaling [2-3]. Tauro-β-muricholic Acid is primarily used in cholestasis research [4].
In Ntcp-HepG2 cells, Co-culture with Tauro-β-muricholic Acid (25μM; 4h) can reduce the cell apoptosis rate to 49% [5]. In STC-1 cells, Tauro-β-muricholic Acid (100-600μM; 24h) treatment triggered a dose-dependent increase in GLP-1 secretion [6].
In Bsep−/− mice, Tauro-β-muricholic Acid (150-600nmol/min; iv; 30min, 60min) infusion increased bile salt secretion [7]. In C70-KO mice, Oral administration of Tauro-β-muricholic Acid (500mg/kg; po; 8 weeks) can reduce the incidence of chronic biliary cholangitis in mice by 40% [8].
References:
[1]. Kuribayashi H, Miyata M, Yamakawa H, et al. Enterobacteria-mediated deconjugation of taurocholic acid enhances ileal farnesoid X receptor signaling[J]. European journal of pharmacology, 2012, 697(1-3): 132-138.
[2]. Miyata M, Tanaka T, Takahashi K, et al. Cholesterol-lowering effects of taurine through the reduction of ileal FXR signaling due to the alteration of ileal bile acid composition[J]. Amino acids, 2021, 53(10): 1523-1532.
[3]. Rau M, Stieger B, Monte M J, et al. Alterations in enterohepatic Fgf15 signaling and changes in bile acid composition depend on localization of murine intestinal inflammation[J]. Inflammatory Bowel Diseases, 2016, 22(10): 2382-2389.
[4]. Zhao D S, Jiang L L, Fan Y X, et al. Identification of urine tauro-β-muricholic acid as a promising biomarker in Polygoni Multiflori Radix-induced hepatotoxicity by targeted metabolomics of bile acids[J]. Food and chemical toxicology, 2017, 108: 532-542.
[5]. Denk G U, Kleiss C P, Wimmer R, et al. Tauro-β-muricholic acid restricts bile acid-induced hepatocellular apoptosis by preserving the mitochondrial membrane potential[J]. Biochemical and biophysical research communications, 2012, 424(4): 758-764.
[6]. Xie Z, Jiang H, Liu W, et al. The triterpenoid sapogenin (2α-OH-Protopanoxadiol) ameliorates metabolic syndrome via the intestinal FXR/GLP-1 axis through gut microbiota remodelling[J]. Cell Death & Disease, 2020, 11(9): 770.
[7]. Gooijert K E R, Havinga R, Wolters H, et al. The mechanism of increased biliary lipid secretion in mice with genetic inactivation of bile salt export pump[J]. American Journal of Physiology-Gastrointestinal and Liver Physiology, 2015, 308(5): G450-G457.
[8]. Chen H, Jiang X, Li Y, et al. A Gallbladder‐Specific Hydrophobic Bile Acid‐FXR‐MUC1 Signaling Axis Mediates Cholesterol Gallstone Formation[J]. Advanced Science, 2025, 12(13): 2401956.
Tauro-β-muricholic Acid (sodium salt)是一种可逆的竞争性法尼基X受体（FXR）拮抗剂（IC50 = 40μM) [1]。Tauro-β-muricholic Acid竞争性抑制FXR活化，从而干扰FXR-SHP和FXR-FGF15通路，增强胆汁酸合成并调节相关的代谢信号传导 [2-3]。Tauro-β-muricholic Acid主要用于胆汁淤积研究 [4]。
在Ntcp-HepG2细胞中，与Tauro-β-muricholic Acid（25μM；4h）共培养可使细胞凋亡率降低至49% [5]。在STC-1细胞中，Tauro-β-muricholic Acid 100-600μM；24h）处理可引发GLP-1分泌的剂量依赖性增加 [6]。
在Bsep−/−小鼠中，输注Tauro-β-muricholic Acid（150-600nmol/min；iv；30min，60min）可增加胆汁盐的分泌 [7]。在C70-KO小鼠中，口服Tauro-β-muricholic Acid（500mg/kg；po；8周）可使小鼠慢性胆汁性胆管炎的发病率降低40% [8]。
| Cell experiment [1]: | |
Cell lines | Ntcp-HepG2 cells |
Preparation Method | Cells were cultured in minimal essential medium (MEM) from PAA supplemented with 10% fetal calf serum, 2mM L-glutamine, 1mM Na-pyruvate, non-essential amino acids (1% of a 100 stock solution), 100U/mL penicillin, 0.1g/L streptomycin,and 1g/L G418 sulfate. After 24h of culture Ntcp-HepG2 cells were incubated for another 4h with the bile acids GCDCA, TUDCA, or Tauro-β-muricholic acid alone, or with combinations of GCDCA + TUDCA or GCDCA + Tauro-β-muricholic Acid, at concentrations of 25μM each, or with the solvent DMSO (0.1%) as control. In addition, cells were incubated with the free fatty acid palmitate 200μM) alone or in the combination with Tauro-β-muricholic Acid. |
Reaction Conditions | 25μM; 4h |
Applications | Co-culture with Tauro-β-muricholic Acid can reduce the cell apoptosis rate to 49%. |
| Animal experiment [2]: | |
Animal models | Bsep−/− mice |
Preparation Method | Bsep−/− mice (n = 7, 4 males; and n = 10, 4 males, respectively; aged 2-5 months) were anesthetized with an intraperitoneal injection of Hypnorm (fentanyl/fluanisol, 1ml/kg) and diazepam (10mg/kg). Bile was collected via gallbladder cannulation. After 5 minutes of equilibration, bile was collected in 30-minute fractions for an additional 90 minutes, representing basal (unstimulated) bile production. The preserved β-muricholic acid secretion was used to analyze the mechanism of BS-induced bile lipid secretion in Bsep−/− mice. To this end, after an initial 90 minutes of (unstimulated) bile collection, Tauro-β-muricholic acid (70mM phosphate buffer) was infused via the jugular vein in escalating doses over 2.5 hours. Tauro-β-muricholic Acid was infused at rates of 150, 300, and 450nmol/min for 30 minutes each, followed by 600nmol/min for 60 minutes. |
Dosage form | 150-600nmol/min; iv; 30min, 60min |
Applications | Tauro-β-muricholic Acid infusion increased bile salt secretion. |
References: | |
| Cas No. | 145022-92-0 | SDF | |
| 别名 | 牛磺-Α-鼠胆酸,Tauro-β-muricholate； TβMCA | ||
| 化学名 | 2-[[(3α,5β,6β,7β)-3,6,7-trihydroxy-24-oxocholan-24-yl]amino]-ethanesulfonic acid, monosodium salt | ||
| Canonical SMILES | C[C@H](CCC(NCCS([O-])(=O)=O)=O)[C@@]1([H])CC[C@@]2([H])[C@]3([H])[C@@H](O)[C@@H](O)[C@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC[C@@]21C.[Na+] | ||
| 分子式 | C26H44NO7S • Na | 分子量 | 537.7 |
| 溶解度 | 1mg/ml in ethanol, 10mg/ml in DMSO & DMF | 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 | 1.8598 mL | 9.2989 mL | 18.5977 mL |
| 5 mM | 372 μL | 1.8598 mL | 3.7195 mL |
| 10 mM | 186 μL | 929.9 μL | 1.8598 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
