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Ursodiol

(Synonyms: 熊去氧胆酸; Ursodeoxycholate; Ursodiol; UDCA)

目录号: PC14956 纯度: ≥98%

用于PBC治疗的胆汁酸，Ursodiol能降低胆固醇吸收，可作用于胆结石的溶解。

CAS No. :128-13-2

商品编号	规格	价格	会员价
PC14956-1g	1g	¥535.00	请登录
PC14956-5g	5g	¥1121.00	请登录
PC14956-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥637.00	请登录

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中文名称

Ursodiol

中文别名

熊去氧胆酸;3alpha,7beta-二羟基-5beta-胆甾烷-24-酸;熊脱氧胆酸;熊果去氧胆酸;乌索去氧胆酸;乌索脱氧胆酸;熊去氧胆酸 GMP;巯基丁酸;熊去氧胆酸 EP标准品;熊去氧胆酸 USP标准品;熊去氧胆酸(UDCA);熊去氧胆酸,BR;熊去氧胆酸,对照品;熊去氧胆酸-[D4]氘代同位素内标;熊去氧胆酸系统适应性 EP标准品;熊脱氧胆酸1;异去氧胆酸;3α,7β-二羟基-5β-胆甾烷-24-酸;尿素;3β,6α-二羟基胆烷酸;二羟基胆基酸;二羟基胆烷酸;猪脱氧胆酸;优思弗;熊去鹅胆酸;熊去氧胆酸标准品;熊去氧胆酸,99%;熊去氧胆酸厂家生产

英文名称

Ursodiol

英文别名

Ursodeoxycholic acid;3A,7B-DIHYDROXY-5B-CHOLAN-24-OIC ACID;3ALPHA,7BETA-DIHYDROXY-5BETA-CHOLAN-24-OIC ACID;3ALPHA, 7BETA-DIHYDROXY-5BETA-CHOLANIC ACID;3ALPHA, 7BETA-DIOXYCHOLANIC ACID;5BETA-CHOLAN-24-OIC ACID-3ALPHA, 7BETA-DIOL;5BETA-CHOLANIC ACID-3ALPHA,7BETA-DIOL;6BETA-CHOLANIC ACID-3A,7BETA-DIOL;(6-BETA)-CHOLANIC ACID-(3-ALPHA)-(7-BETA)-DIOL;7BETA-HYDROXYLITHOCHOLIC ACID;UDCA;UDCS;URSODEOXYCHOLOC ACID;17-beta-(1-methyl-3-carboxypropyl)etiocholane-3-alpha,7-beta-diol;3,7-dihydroxy-,(3-alpha,5-beta,7-beta)-cholan-24-oicaci;3-alpha,7-beta-dihydroxy-5-beta-cholan-24-oicaci;5B-CHOLANIC ACID-3A,7A-DIOL;URSODEOXYCHOLIC ACID(RG);(4R)-4-[(3R,5S,7S,8R,9S,10S,13R,14S,17R)-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoic acid;3α,7β-Dihydroxy-5β-cholan-24-oic acid;3α,7β-Dihydroxy-5β-cholanic Acid;5β-Cholan-24-oic acid-3α,7β-diol;5β-Cholanic Acid-3α,7β-diol;7β-Hydroxylithocholic acid;Urea;URSODEOXYCHOLIC ACID ,EP5;Tauroursodiol;3,7-Dihydroxycholan-24-oic acid;3alpha,7beta-Dihydroxy-6beta-cholan-24-oic acid;Ursodiol;urso;Desol;Urdes;lyeton;arsacol;deursil;ursacol;Desocol;Actigall;Ursolvan;Ursofalk;Delursan;Urso Forte;Ursodesoxycholic acid;Destolit;Ursochol;ursodeoxycholate;Cholit-ursan;Ursobilin;Litursol;Ursodamor;Solutrat;Peptarom;Urso DS;Ursosan;Ursodexycholic Acid;Urso 250;7-beta-Hydroxylithocholic acid;Acido ursodeoxicolico;Antigall;Acido ursodeossicolico;Acidum ursodeoxycholicum;Acide ursodesoxycholique;3-alpha,7-beta-Dioxycho

Cas No.

128-13-2

分子式

C₂₄H₄₀O₄

分子量

392.57

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

详情描述

用于PBC治疗的胆汁酸，Ursodiol能降低胆固醇吸收，可作用于胆结石的溶解。

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 reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection. Orally active.

性状

Solid

IC50 & Target[1][2]

Human Endogenous Metabolite

FATP5

ACE2

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Ursodeoxycholic acid (1% w/w or 416 mg/kg; oral; 7 days) reduces ACE2 expression in mice and hamsters.
Ursodeoxycholic acid (416 mg/kg; oral; 7 days) reduces SARS-CoV-2 infection in hamsters.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	5 week old C57BL/6J WT mice (male and female)
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
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
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).

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

结构分类

Steroids

参考文献

[1]. Jackson H, et al. Influence of ursodeoxycholic acid on the mortality and malignancy associated with primary biliary cirrhosis: a population-based cohort study. Hepatology. 2007 Oct;46(4):1131-7. [Information]

[2]. Kumar D, et al. Use of ursodeoxycholic acid in liver diseases. J Gastroenterol Hepatol. 2001 Jan;16(1):3-14. [Information]

[3]. Biao Nie, et al. Specific Bile Acids Inhibit Hepatic Fatty Acid Uptake in Mice. Hepatology. 2012 Oct;56(4):1300-10. [Information]

[4]. Brevini T, et al. FXR inhibition may protect from SARS-CoV-2 infection by reducing ACE2. Nature. 2022 Dec 5. [Information]

溶解度数据

体外研究:

DMSO : ≥ 100 mg/mL (254.73 mM)

H₂O : 1 mg/mL (2.55 mM; ultrasonic and warming and heat to 80°C)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 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。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Ursodiol

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