1. GPCR/G Protein Metabolic Enzyme/Protease
  2. G protein-coupled Bile Acid Receptor 1 FXR Angiotensin-converting Enzyme (ACE) Endogenous Metabolite
  3. Ursodeoxycholic acid

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

目录号: HY-13771 纯度: ≥98.0%
COA 产品使用指南

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。

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Ursodeoxycholic acid Chemical Structure

Ursodeoxycholic acid Chemical Structure

CAS No. : 128-13-2

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10 mM * 1 mL in DMSO ¥500
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Other Forms of Ursodeoxycholic acid:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1][2][3][4].

IC50 & Target[3][4]

Human Endogenous Metabolite

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 200 μM
Compound: UDCA
Anticancer activity against human A549 cells assessed as inhibition of cell proliferation by MTT assay
Anticancer activity against human A549 cells assessed as inhibition of cell proliferation by MTT assay
[PMID: 36439975]
CHO EC50
36.4 μM
Compound: 9, UDCA
Agonist activity at human TGR5 expressed in CHO cells by luciferase assay
Agonist activity at human TGR5 expressed in CHO cells by luciferase assay
[PMID: 18307294]
COS-1 EC50
> 50 μM
Compound: 9, UDCA
Agonist activity at human FXR expressed in COS1 cells by luciferase assay
Agonist activity at human FXR expressed in COS1 cells by luciferase assay
[PMID: 18307294]
GBM IC50
> 50 μM
Compound: 1b, UDCA, ursodeoxycholic acid
Cytotoxicity against human GBM cells after 24 hrs by neutral red uptake assay
Cytotoxicity against human GBM cells after 24 hrs by neutral red uptake assay
[PMID: 20381215]
HCT-116 IC50
> 200 μM
Compound: UDCA
Anticancer activity against human HCT-116 cells assessed as inhibition of cell proliferation by MTT assay
Anticancer activity against human HCT-116 cells assessed as inhibition of cell proliferation by MTT assay
[PMID: 36439975]
HCT-116 IC50
> 50 μM
Compound: 1b, UDCA, ursodeoxycholic acid
Cytotoxicity against human HCT116 cells after 24 hrs by neutral red uptake assay
Cytotoxicity against human HCT116 cells after 24 hrs by neutral red uptake assay
[PMID: 20381215]
HEK293 EC50
2.39 μM
Compound: 3, UDCA
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
[PMID: 25735208]
HEK-293T EC50
> 150 μM
Compound: UDCA
Agonist activity at VP16 tagged-VDR-LBD (unknown origin) expressed in HEK293T cells assessed as SRC1 coactivator peptide recruitment after 16 hrs by luciferase reporter gene based two hybrid assay
Agonist activity at VP16 tagged-VDR-LBD (unknown origin) expressed in HEK293T cells assessed as SRC1 coactivator peptide recruitment after 16 hrs by luciferase reporter gene based two hybrid assay
[PMID: 26774929]
HEK-293T IC50
> 50 μM
Compound: UDCA
Antagonist activity against VP16 tagged-VDR-LBD (unknown origin) expressed in HEK293T cells assessed as inhibition of 1,25-dihydroxyvitamin D3-induced SRC1 coactivator peptide recruitment after 16 hrs by luciferase reporter gene based two hybrid assay
Antagonist activity against VP16 tagged-VDR-LBD (unknown origin) expressed in HEK293T cells assessed as inhibition of 1,25-dihydroxyvitamin D3-induced SRC1 coactivator peptide recruitment after 16 hrs by luciferase reporter gene based two hybrid assay
[PMID: 26774929]
HET-1A CC50
1313 μM
Compound: 7, UDCA
Cytotoxicity against human HET-1A cells assessed as cell viability after 24 hrs by MTT assay
Cytotoxicity against human HET-1A cells assessed as cell viability after 24 hrs by MTT assay
[PMID: 20713311]
HT-29 IC50
> 200 μM
Compound: UDCA
Anticancer activity against human HT-29 cells assessed as inhibition of cell proliferation by MTT assay
Anticancer activity against human HT-29 cells assessed as inhibition of cell proliferation by MTT assay
[PMID: 36439975]
Huh-7 IC50
> 200 μM
Compound: UDCA
Anticancer activity against human Huh-7 cells assessed as inhibition of cell proliferation by MTT assay
Anticancer activity against human Huh-7 cells assessed as inhibition of cell proliferation by MTT assay
[PMID: 36439975]
KMS-11 IC50
> 50 μM
Compound: 1b, UDCA, ursodeoxycholic acid
Cytotoxicity against human KMS11 cells after 24 hrs by neutral red uptake assay
Cytotoxicity against human KMS11 cells after 24 hrs by neutral red uptake assay
[PMID: 20381215]
LoVo IC50
> 200 μM
Compound: UDCA
Anticancer activity against human LoVo cells assessed as inhibition of cell proliferation by MTT assay
Anticancer activity against human LoVo cells assessed as inhibition of cell proliferation by MTT assay
[PMID: 36439975]
MGC-803 IC50
> 200 μM
Compound: UDCA
Anticancer activity against human MGC-803 cells assessed as inhibition of cell proliferation by MTT assay
Anticancer activity against human MGC-803 cells assessed as inhibition of cell proliferation by MTT assay
[PMID: 36439975]
RKO IC50
> 200 μM
Compound: UDCA
Anticancer activity against human RKO cells assessed as inhibition of cell proliferation by MTT assay
Anticancer activity against human RKO cells assessed as inhibition of cell proliferation by MTT assay
[PMID: 36439975]
SK-HEP1 IC50
> 200 μM
Compound: UDCA
Anticancer activity against human SK-HEP1 cells assessed as inhibition of cell proliferation by MTT assay
Anticancer activity against human SK-HEP1 cells assessed as inhibition of cell proliferation by MTT assay
[PMID: 36439975]
SW480 IC50
> 200 μM
Compound: UDCA
Anticancer activity against human SW480 cells assessed as inhibition of cell proliferation by MTT assay
Anticancer activity against human SW480 cells assessed as inhibition of cell proliferation by MTT assay
[PMID: 36439975]
体外研究
(In Vitro)

Ursodeoxycholic acid (10 μM;24 小时) 降低初级气道和肠道类器官中的 ACE2 和 SHP 水平,并通过 FXR 介导的 ACE2 调节减少多种细胞类型中的 SARS-CoV-2 感染[4]

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

体内研究
(In Vivo)

Ursodeoxycholic acid (10 μM;24 小时) 降低初级气道和肠道类器官中的 ACE2 和 SHP 水平,并通过 FXR 介导的 ACE2 调节减少多种细胞类型中的 SARS-CoV-2 感染[4]

MCE 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)[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).
分子量

392.57

Formula

C24H40O4

CAS 号
性状

固体

颜色

White to off-white

中文名称

熊去氧胆酸

结构分类
初始来源
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
溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 100 mg/mL (254.73 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

配制储备液
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
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

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

  • 方案 一

    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); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (5.30 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    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。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: ≥98.0%

参考文献

完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5473 mL 12.7366 mL 25.4732 mL 63.6829 mL
5 mM 0.5095 mL 2.5473 mL 5.0946 mL 12.7366 mL
10 mM 0.2547 mL 1.2737 mL 2.5473 mL 6.3683 mL
15 mM 0.1698 mL 0.8491 mL 1.6982 mL 4.2455 mL
20 mM 0.1274 mL 0.6368 mL 1.2737 mL 3.1841 mL
25 mM 0.1019 mL 0.5095 mL 1.0189 mL 2.5473 mL
30 mM 0.0849 mL 0.4246 mL 0.8491 mL 2.1228 mL
40 mM 0.0637 mL 0.3184 mL 0.6368 mL 1.5921 mL
50 mM 0.0509 mL 0.2547 mL 0.5095 mL 1.2737 mL
60 mM 0.0425 mL 0.2123 mL 0.4246 mL 1.0614 mL
80 mM 0.0318 mL 0.1592 mL 0.3184 mL 0.7960 mL
100 mM 0.0255 mL 0.1274 mL 0.2547 mL 0.6368 mL
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Ursodeoxycholic acid
目录号:
HY-13771
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