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

Ursodeoxycholic acid  (Synonyms: 熊去氧膽酸; Ursodeoxycholate; Ursodiol; UDCA)

目錄號(hào): HY-13771 純度: ≥98.0%
COA 產(chǎn)品使用指南

Ursodeoxycholic acid (Ursodeoxycholate) 是由腸道細(xì)菌轉(zhuǎn)化 (cheno) 脫氧膽酸而產(chǎn)生的一種次級(jí)膽汁酸，是腸道屏障完整性的關(guān)鍵調(diào)節(jié)因子，對(duì)脂質(zhì)代謝至關(guān)重要。Ursodeoxycholic acid 作為信號(hào)分子，通過(guò)與膽汁酸激活的受體相互作用發(fā)揮作用，包括 G 蛋白偶聯(lián)的膽汁酸受體 5 (TGR5, GPCR19) 和法尼酯 X 受體 (FXR)。Ursodeoxycholic acid 可用于多種肝臟和胃腸道疾病的研究。Ursodeoxycholic acid 也減少 ACE2 的表達(dá)，有助于減少 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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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥500
In-stock
500 mg ￥350
In-stock
1 g ￥400
In-stock
5 g ￥930
In-stock
10 g   詢(xún)價(jià)  
50 g   詢(xún)價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Ursodeoxycholic acid:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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

 

細(xì)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]
體外研究
(In Vitro)

Ursodeoxycholic acid (10 μM；24 小時(shí)) 降低初級(jí)氣道和腸道類(lèi)器官中的 ACE2 和 SHP 水平，并通過(guò) FXR 介導(dǎo)的 ACE2 調(diào)節(jié)減少多種細(xì)胞類(lèi)型中的 SARS-CoV-2 感染[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

Ursodeoxycholic acid (10 μM；24 小時(shí)) 降低初級(jí)氣道和腸道類(lèi)器官中的 ACE2 和 SHP 水平，并通過(guò) FXR 介導(dǎo)的 ACE2 調(diào)節(jié)減少多種細(xì)胞類(lèi)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 號(hào)
性狀

固體

顏色

White to off-white

中文名稱(chēng)

熊去氧膽酸
結(jié)構(gòu)分類(lèi)
初始來(lái)源
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : ≥ 100 mg/mL (254.73 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

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

    此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: ≥98.0%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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
Help & FAQs
  • Do most proteins show cross-species activity?

    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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產(chǎn)品名稱(chēng)：
Ursodeoxycholic acid
目錄號(hào)：
HY-13771
需求量：