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Ursodeoxycholic acid

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纯度: 99.91%

货号 T0700Cas号 128-13-2

别名 熊去氧胆酸, Ursodiol, UDCA

Ursodeoxycholic acid (UDCA) 是一种有效的肝脏特异性脂肪酸转运蛋白 5 (FATP5) 抑制剂。Ursodeoxycholic acid 能够抑制胆固醇的吸收,用于溶解胆结石。

Ursodeoxycholic acid

Ursodeoxycholic acid

一键复制产品信息
Rating icon 很棒

纯度: 99.91%

货号 T0700 别名 熊去氧胆酸, Ursodiol, UDCACas号 128-13-2

Ursodeoxycholic acid (UDCA) 是一种有效的肝脏特异性脂肪酸转运蛋白 5 (FATP5) 抑制剂。Ursodeoxycholic acid 能够抑制胆固醇的吸收,用于溶解胆结石。

规格价格库存数量
500 mg
¥ 275
现货
1 g
¥ 333
现货
5 g
¥ 781
现货
1 mL x 10 mM (in DMSO)
¥ 415
现货
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产品介绍


Ursodeoxycholic acid AI Summary
Ursodeoxycholic acid is a multifaceted chemical with a wide spectrum of bioactivities and evaluated physico-chemical properties. It demonstrates a high binding constant of 173,400.0 Kb M-1 towards a cyclodextrin conjugated peptide with pyrene at 25°C and exhibits a sensitivity change of 0.4 at this temperature. Its critical micellar concentration (CMC) is reported to be 19.0 mM, with a pKa value of 5.08 and water solubility at 9000.0 nM. The compound shows a Percent Hepatic Uptake of 50.0%, an Albumin Affinity Constant of 38,000.0 L M-1, and significant effects on bile flow and secretion of bile acids, cholesterol, and phospholipids in bile fistula rats. It activates the human PXR receptor, displays agonist activity at the human TGR5 receptor, and shows significant interactions with the human GPBAR1 and various nuclear receptors. Ursodeoxycholic acid has moderate lipophilicity (LogP = 4.014) and demonstrates varied effects on liver enzymes, with moderate hepatotoxicity observed in clinical trials. It inhibits glucuronosyltransferase activity in human colon cancer cells (HT-29) and shows potent inhibitory effects on several human tumor cell lines and Plasmodium falciparum M1-Family Alanyl Aminopeptidase. It modulates bile salt export pump (BSEP) and Taurocholate transport, and exhibits hepatoprotective activity in mice on a lithogenic diet, reducing gallstone formation and serum cholesterol levels. The compound shows modest antiviral activity against SARS-CoV-2, with some inhibition of the virus's 3CL-Pro protease and induced cytotoxicity in various cell lines. It has also exhibited antifungal activity against Candida albicans and Cryptococcus neoformans and antibacterial properties against several bacterial strains including Escherichia coli and Staphylococcus aureus MRSA. Despite the diverse bioactivity profile, Ursodeoxycholic acid does not induce significant drug-induced liver injury, has no cytotoxic impact against human HepG2 and Hep3B cells at low concentrations, and shows a varied efficacy when tested for anticancer activities on numerous human cell lines. Overall, Ursodeoxycholic acid demonstrates potential therapeutic applications across a broad range of biological targets and disease models, underscoring its significance in pharmaceutical research..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Ursodeoxycholic acid (UDCA) is a potent inhibitor of liver-specific fatty acid transporter 5 (FATP5). Ursodeoxycholic acid inhibits cholesterol absorption and is used to dissolve gallstones.
靶点活性
CHO cells:36.4 μM (EC50), A549 cells:> 200 μM, GBM:> 50 μM
体外活性

方法:卵巢癌细胞A2780和顺铂耐药的A2780细胞用Ursodeoxycholic acid(300 nM)处理4小时,使用MTT方法检测细胞生长抑制情况。
结果:Ursodeoxycholic acid抑制卵巢癌细胞A2780(IC50=300 nM)和顺铂耐药的A2780细胞(IC50=300 nM)生长。[1]
方法:结直肠癌细胞SW620和HCT116用Ursodeoxycholic acid(0、0.00625、0.0125、0.025、0.05、0.1 mg/mL)处理24小时,使用MTT方法检测细胞生长抑制情况。
结果:Ursodeoxycholic acid抑制结直肠癌细胞SW620(IC50=0.02 mg/mL)和HCT116(IC50=0.016 mg/mL)生长。[2]

体内活性

方法:为研究Ursodeoxycholic acid对体重的影响,将Ursodeoxycholic acid(50、 150、 450 mg/kg)口服给小鼠,连续21天。
结果:在接受50和450 mg/kg剂量的小鼠组中,一周内显著体重减轻。在50 mg/kg剂量下,这种体重减轻在整个实验过程中持续存在。在450 mg/kg剂量下,最初在Ursodeoxycholic acid给药的第一周和第三周观察到体重减轻。在150 mg/kg剂量下,与未治疗的小鼠相比,体重没有显著差异。[3]

别名熊去氧胆酸, Ursodiol, UDCA
化学信息
分子量392.57
分子式C24H40O4
CAS No.128-13-2
SmilesC[C@@]12[C@]([C@]3([C@@]([C@]4(C)[C@](C[C@@H]3O)(C[C@H](O)CC4)[H])(CC1)[H])[H])(CC[C@@]2([C@@H](CCC(O)=O)C)[H])[H]
密度1.128 g/cm3.
颜色White
物理性状Solid
储存&溶解度
存储keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度信息
Ethanol: 73 mg/mL (185.95 mM), Sonication is recommended.
DMSO: 255 mg/mL (649.57 mM), Sonication is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (12.74 mM), Sonication is recommended.
请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。
溶液配制表
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.5473 mL12.7366 mL25.4732 mL127.3658 mL
5 mM0.5095 mL2.5473 mL5.0946 mL25.4732 mL
10 mM0.2547 mL1.2737 mL2.5473 mL12.7366 mL
20 mM0.1274 mL0.6368 mL1.2737 mL6.3683 mL
50 mM0.0509 mL0.2547 mL0.5095 mL2.5473 mL
100 mM0.0255 mL0.1274 mL0.2547 mL1.2737 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments 比如您的给药剂量是10 mg/kg,每只动物体重20g,给药体积100 μLTargetMol | Animal experiments 一共给药动物10只,您使用的配方为5%TargetMol | reagent DMSO + 30%PEG300 + 5%Tween 80 + 60%Saline/PBS/ddH2O, 那么您的工作液浓度为2mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween80, 混匀澄清,再加 600μLSaline/PBS/ddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

方案所需的各类助溶剂如: DMSOPEG300 / PEG400Tween 80SBE-β-CD玉米油 等, 均可在TargetMol网站点击购买。
1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

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