Ursodeoxycholic acid (Ursodeoxycholate) 是由肠道细菌转化 (cheno) 脱氧胆酸而产生的一种次级胆汁酸，是肠道屏障完整性的关键调节因子，对脂质代谢至关重要。Ursodeoxycholic acid 作为信号分子，通过与胆汁酸激活的受体相互作用发挥作用，包括 G 蛋白偶联的胆汁酸受体 5 (TGR5,GPCR19) 和法尼酯 X 受体 (FXR)。Ursodeoxycholic acid 可用于多种肝脏和胃肠道疾病的研究。Ursodeoxycholic acid 也减少ACE2的表达，有助于减少SARS-CoV-2感染 。具有口服活性。
| 生物活性 | Ursodeoxycholic acid (Ursodeoxycholate) is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5,GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Ursodeoxycholic acid also reducesACE2expression and is beneficial for reducingSARS-CoV-2infection. Orally active[1][2][3][4]. |
| IC50& Target[3][4] | Human Endogenous Metabolite | FATP5 | ACE2 |
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体外研究
(In Vitro) | Ursodeoxycholic acid (10 μM; 24 h) reduces ACE2 and SHP levels in primary airway and intestinal organoids, and reduces SARS-CoV-2 infection in multiple cell types via FXR-mediated ACE2 regulation[4].
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体内研究
(In Vivo) | Ursodeoxycholic acid (50, 150, and 450 mg/kg; p.o.; daily for 21 days) results in weight loss in C57BL/6J wildtype mice[1].
Ursodeoxycholic acid (1% w/w or 416 mg/kg; oral; 7 days) reduces ACE2 expression in mice and hamsters[4].
Ursodeoxycholic acid (416 mg/kg; oral; 7 days) reduces SARS-CoV-2 infection in hamsters[4].
| Animal Model: | 5 week old C57BL/6J WT mice (male and female)[1] | | Dosage: | 50, 150, and 450 mg/kg dissolved in corn oil | | Administration: | Oral gavage; daily for 21 days | | Result: | Mice in the 50 and 450 mg/kg groups sustained significant weight loss within a week. At 50 mg/kg, this weight loss persisted over the course of the experiment. At 450 mg/kg, initially weight loss was noted during the first and third week of ursodiol administration. At 150 mg/kg, it did not have significantly different weights compared to the untreated mice. |
| Animal Model: | FVB/N mice and Syrian Golden Hamsters[4] | | Dosage: | 1% w/w for mice, 416 mg/kg for hamsters | | Administration: | In chow or oral gavage, 7 days | | Result: | Reduced ACE2 expression. |
| Animal Model: | Syrian Golden Hamsters, SARS-CoV-2 infection model[4] | | Dosage: | 416 mg/kg | | Administration: | Oral gavage, 7 days | | Result: | Prevented transmission of SARS-CoV-2 in n=6 out of 9 sentinel animals (33% infected vs. 67% uninfected). |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(254.73 mM) H2O : 1 mg/mL(2.55 mM;ultrasonic and warming and heat to 80℃) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.5473 mL | 12.7366 mL | 25.4732 mL | | 5 mM | 0.5095 mL | 2.5473 mL | 5.0946 mL | | 10 mM | 0.2547 mL | 1.2737 mL | 2.5473 mL |
*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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.30 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.30 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.30 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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