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Tauroursodeoxycholate sodium

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Chemical Structure| 35807-85-3 同义名 : 牛磺熊脱氧胆酸钠 ;Tauroursodeoxycholic acid sodium;UR 906 sodium;Ursodeoxycholyltaurine sodium;TUDC;Sodium Tauroursodeoxycholate;TUDCA sodium
CAS号 : 35807-85-3
货号 : A154752
分子式 : C26H45NNaO6S
纯度 : 99%+
分子量 : 522.693
MDL号 : -
存储条件:

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(200.88 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 100 mg/mL(191.32 mM),配合低频超声助溶

动物实验配方:

PO 0.5% CMC-Na 35 mg/mL clear

生物活性
描述 Tauroursodeoxycholate Sodium is a water-soluble bile acid used in the treatment of gallstones and cirrhosis. Tauroursodeoxycholate (TUDC) is well known to protect against glycochenodeoxycholate (GCDC)-induced apoptosis in rat hepatocytes. While GCDC upregulated the expression of several pro-inflammatory genes, co-perfusion with TUDC increased the expression of pro-proliferative and anti-apoptotic p53 target genes[3]. 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. 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 (myeloperoxidase) 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[4]. Tauroursodeoxycholate (360 μ mol / kg, i.v.) significantly inhibited the decrease of bile flow and increased the activities of serum alkaline phosphatase, leucine aminopeptidase and alanine aminotransferase, as well as the concentrations of cholesterol, phospholipids and bile acids in rats with bile obstruction induced by phalloidin[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03127514 Amyotrophic Lateral Sclerosis ... 展开 >> Motor Neuron Disease Neuromuscular Diseases Neurodegenerative Diseases Spinal Cord Diseases TDP-43 Proteinopathies Nervous System Diseases Central Nervous System Diseases 收起 << Phase 2 Recruiting May 2019 -
NCT00771901 - Completed - -
NCT03533257 Alzheimer Disease Phase 2 Recruiting September 1, 2020 United States, Illinois ... 展开 >> Rush University Medical Center Recruiting Chicago, Illinois, United States, 60612 Contact: Judy Phillips    312-942-0050    Judy_Phillips@rush.edu    United States, Kansas University of Kansas Clinical Research Center Recruiting Fairway, Kansas, United States, 66205 Contact: KUMC Recruitment Division    913-588-0555    KUAMP@kumc.edu    United States, Massachusetts Massachusetts General Hospital Recruiting Boston, Massachusetts, United States, 02114 Contact: Alison J McManus, DNP    617-643-4848    ajmcmanus@mgh.harvard.edu    Contact: John Ernandez    617-643-4047    jernandez@partners.org    United States, New Jersey Rowan University Not yet recruiting Stratford, New Jersey, United States, 08084 Contact: Lauren Fedor    856-566-6003    fedor@rowan.edu    United States, New York Mount Sinai Alzheimer's Disease Research Center Not yet recruiting New York, New York, United States, 10029 Contact: Caroline Meuser    212-659-8885    caroline.meuser@mssm.edu    Columbia University Recruiting New York, New York, United States, 10032 Contact: Ruth Tejeda    212-305-7661    rbt41@cumc.columbia.edu    United States, Pennsylvania Penn Memory Center Recruiting Philadelphia, Pennsylvania, United States, 19104 Contact: Laura Schankel    215-349-8727    laura.schankel@pennmedicine.upenn.edu 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.91mL

0.38mL

0.19mL

9.57mL

1.91mL

0.96mL

19.13mL

3.83mL

1.91mL

参考文献

[1]Alpini G, Kanno N, et al. Tauroursodeoxycholate inhibits human cholangiocarcinoma growth via Ca2+-, PKC-, and MAPK-dependent pathways. Am J Physiol Gastrointest Liver Physiol. 2004 Jun;286(6):G973-82.

[2]Milkiewicz P, Roma MG, et al. Effect of tauroursodeoxycholate and S-adenosyl-L-methionine on 17beta-estradiol glucuronide-induced cholestasis. J Hepatol. 2001 Feb;34(2):184-91.

[3]Paluschinski M, Castoldi M, Schöler D, Bardeck N, Oenarto J, Görg B, Häussinger D. Tauroursodeoxycholate protects from glycochenodeoxycholate-induced gene expression changes in perfused rat liver. Biol Chem. 2019 Nov 26;400(12):1551-1565

[4]Yang Y, He J, Suo Y, Zheng Z, Wang J, Lv L, Huo C, Wang Z, Li J, Sun W, Zhang Y. Tauroursodeoxycholate improves 2,4,6-trinitrobenzenesulfonic acid-induced experimental acute ulcerative colitis in mice. Int Immunopharmacol. 2016 Jul;36:271-276

[5]Ishizaki K, Kinbara S, Hirabayashi N, Uchiyama K, Maeda M. Effect of sodium tauroursodeoxycholate on phalloidin-induced cholestasis in rats. Eur J Pharmacol. 2001 Jun 1;421(1):55-60