Obeticholic acid (Synonyms: 奥贝胆酸; INT-747; 6-ECDCA; 6-Ethylchenodeoxycholic acid)

目录号: HY-12222 纯度: ≥98.0%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Obeticholic acid (INT-747) 是一种有效的，选择性的和口服活性的 FXR 激动剂，EC₅₀ 为 99 nM，并具有抗胆碱和抗炎作用。Obeticholic acid 还可诱导细胞自噬 (autophagy)。

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Obeticholic acid Chemical Structure

CAS No. : 459789-99-2

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥600	In-stock
5 mg	￥550	In-stock
10 mg	￥1000	In-stock
20 mg	￥1550	In-stock
50 mg	￥2800	In-stock
100 mg	￥4700	In-stock
500 mg		询价

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Other Forms of Obeticholic acid:

MCE 顾客使用本产品发表的 66 篇科研文献

: Obeticholic acid purchased from MCE. Usage Cited in: J Am Soc Nephrol. 2018 Nov;29(11):2658-2670. [Abstract]; Western blots show that INT-767, INT-777, and INT747 upregulate AQP2 protein expression.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC₅₀ of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy^[1]^[2]^[3].

IC₅₀ & Target

EC50: 99 nM (FXR)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CHO	EC₅₀	0.755 μM Compound: 1, 6ECDCA	Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay	[PMID: 17685603]
COS-1	EC₅₀	0.099 μM Compound: 5, 6-ECDCA, INT-747	Agonist activity at FXR expressed in COS1 cells by cell-based bioluminescence assay Agonist activity at FXR expressed in COS1 cells by cell-based bioluminescence assay	[PMID: 20014870]
COS-1	EC₅₀	0.361 μM Compound: 1, 6ECDCA	Agonist activity at human FXR expressed in COS1 cells after 5 hrs by CRE-driven luciferase reporter gene assay Agonist activity at human FXR expressed in COS1 cells after 5 hrs by CRE-driven luciferase reporter gene assay	[PMID: 17685603]
HEK-293T	EC₅₀	42 nM Compound: OCA; INT-747	Agonist activity at human FXR expressed in HEK293T cells assessed as BSEP promoter driven cellular transcriptional activity after 24 hrs by luciferase reporter gene assay Agonist activity at human FXR expressed in HEK293T cells assessed as BSEP promoter driven cellular transcriptional activity after 24 hrs by luciferase reporter gene assay	[PMID: 29148806]
HeLa	EC₅₀	0.16 μM Compound: 2,6-ECDCA	Agonist activity at human full length FXR expressed in HeLa cells cotransfected with pSG5-human RXR after 24 hrs by Dual-Glo luciferase reporter gene assay Agonist activity at human full length FXR expressed in HeLa cells cotransfected with pSG5-human RXR after 24 hrs by Dual-Glo luciferase reporter gene assay	[PMID: 25934227]
HeLa	EC₅₀	0.16 μM Compound: 2, 6-ECDCA, Obeticholic acid, INT-747	Agonist activity at human FXR expressed in human HeLa cells assessed as receptor activation by BSEP promoter-driven firefly luciferase reporter gene assay Agonist activity at human FXR expressed in human HeLa cells assessed as receptor activation by BSEP promoter-driven firefly luciferase reporter gene assay	[PMID: 25255039]
HepG2	EC₅₀	0.5 μM Compound: 2; 6-ECDCA, INT747, OCA	Transactivation of human FXR (unknown origin) expressed in HepG2 cells co-expressing pSG5RXR/pGL4.70 after 24 hrs post transfection by luciferase reporter gene assay Transactivation of human FXR (unknown origin) expressed in HepG2 cells co-expressing pSG5RXR/pGL4.70 after 24 hrs post transfection by luciferase reporter gene assay	[PMID: 30996771]
NCI-H716	EC₅₀	20 μM Compound: 2, 6-ECDCA, INT-747	Agonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assay Agonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assay	[PMID: 21459580]

体外研究
(In Vitro)

Obeticholic acid (INT-747) 可增加大鼠肝细胞中 FXR 调节基因的表达^[1]。
Obeticholic acid 可降低肝脏 JNK-1 和 JNK-2 的表达^[2]。
Obeticholic acid (256 μg/mL) 可抑制所有测试菌株中的细菌生长。在暴露于 IFN-γ 的 Caco-2 细胞肠上皮中添加 Obeticholic acid 后，肠道通透性不受影响^[3]。

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

体内研究
(In Vivo)

Obeticholic acid (INT-747) (10 mg/kg/天) 缓解了 E₂17α 引起的胆汁淤积。Obeticholic acid 通过增加 β-MCA 和 TCDCA 和 TDCA 的相对含量，可部分预防由 E₂17α 导致的总胆汁酸输出受损^[1]。
Obeticholic acid (10 mg/kg) 和 HS 会增加动物的肺充血情况。Obeticholic acid 不能改善 HS 喂养动物的肾脏病变^[2]。
Obeticholic acid (5 mg/kg) 能显著提高 BDL 大鼠的存活率。Obeticholic acid 大鼠中显著选择性增加回肠闭孔蛋白claudin-1的表达，并显著上调回肠ZO-1的表达^[3]。

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

Clinical Trial

分子量

420.63

Formula

C₂₆H₄₄O₄

CAS 号

459789-99-2

性状

固体

颜色

White to off-white

中文名称

奥贝胆酸；6-乙基鹅去氧胆酸

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 (237.74 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)

Ethanol 中的溶解度 : ≥ 50 mg/mL (118.87 mM)

* "≥" 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	2.3774 mL	11.8869 mL	23.7739 mL
5 mM	0.4755 mL	2.3774 mL	4.7548 mL
10 mM	0.2377 mL	1.1887 mL	2.3774 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (11.89 mM); 澄清溶液

此方案可获得 ≥ 5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 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。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (11.89 mM); 澄清溶液

此方案可获得 ≥ 5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
方案三

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 4.76 mg/mL (11.32 mM); 澄清溶液

此方案可获得 ≥ 4.76 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 47.6 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。
方案四

请依序添加每种溶剂： 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.94 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 EtOH 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。
方案五

请依序添加每种溶剂： 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.94 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 EtOH 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。
方案六

请依序添加每种溶剂： 10% EtOH 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.94 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 玉米油中，混合均匀。
方案七

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.94 mM); 澄清溶液

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。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： 1% Methylcellulose/saline water
Solubility: 5 mg/mL (11.89 mM); Suspension solution; 超声助溶

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

每只动物的给药体积

μL

动物数量

只

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%

选择批次：

Data Sheet (650 KB) SDS (393 KB)

COA (288 KB) HNMR (294 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Pellicciari R, et al. 6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity. J Med Chem. 2002 Aug 15;45(17):3569-72. [Content Brief]

[2]. Fiorucci S, et al. Protective effects of 6-ethyl chenodeoxycholic acid, a farnesoid X receptor ligand, in estrogen-induced cholestasis. J Pharmacol Exp Ther. 2005 May;313(2):604-12. [Content Brief]

[3]. Ghebremariam YT, et al. FXR agonist INT-747 upregulates DDAH expression and enhances sensitivity in high-salt fed Dahl rats. PLoS One. 2013 Apr 4;8(4):e60653. [Content Brief]

[4]. Verbeke L, et al. The FXR Agonist Obeticholic Acid Prevents Gut Barrier Dysfunction and Bacterial Translocation in Cholestatic Rats. Am J Pathol. 2015 Feb;185(2):409-19. [Content Brief]

Animal Administration ^[2]	Initially, all animals (at 6-weeks age) are placed on a standard rodent diet for a week. Baseline blood and urine samples are collected and basal blood pressure (BP) is measured prior to grouping the animals. Subsequently, the animals are randomized into low (LS; n=9) or high salt (HS) diet groups. Hypertension is induced in the HS group by daily high-salt diet feeding and the group is subdivided to receive one of two doses of INT-747: low dose (10 mg/kg/day; n=15) or high dose (30 mg/kg/day; n=15) in 1% methylcellulose; or vehicle (1% methylcellulose in distilled water; n=15) orally everyday for 6 weeks. In parallel, the LS group also receive 1% methylcellulose. BP is measured weekly for the duration of the study as described below. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Pellicciari R, et al. 6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity. J Med Chem. 2002 Aug 15;45(17):3569-72. [Content Brief] [2]. Fiorucci S, et al. Protective effects of 6-ethyl chenodeoxycholic acid, a farnesoid X receptor ligand, in estrogen-induced cholestasis. J Pharmacol Exp Ther. 2005 May;313(2):604-12. [Content Brief] [3]. Ghebremariam YT, et al. FXR agonist INT-747 upregulates DDAH expression and enhances sensitivity in high-salt fed Dahl rats. PLoS One. 2013 Apr 4;8(4):e60653. [Content Brief] [4]. Verbeke L, et al. The FXR Agonist Obeticholic Acid Prevents Gut Barrier Dysfunction and Bacterial Translocation in Cholestatic Rats. Am J Pathol. 2015 Feb;185(2):409-19. [Content Brief]

Animal Administration
^[2]

Initially, all animals (at 6-weeks age) are placed on a standard rodent diet for a week. Baseline blood and urine samples are collected and basal blood pressure (BP) is measured prior to grouping the animals. Subsequently, the animals are randomized into low (LS; n=9) or high salt (HS) diet groups. Hypertension is induced in the HS group by daily high-salt diet feeding and the group is subdivided to receive one of two doses of INT-747: low dose (10 mg/kg/day; n=15) or high dose (30 mg/kg/day; n=15) in 1% methylcellulose; or vehicle (1% methylcellulose in distilled water; n=15) orally everyday for 6 weeks. In parallel, the LS group also receive 1% methylcellulose. BP is measured weekly for the duration of the study as described below.

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

参考文献

[1]. Pellicciari R, et al. 6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity. J Med Chem. 2002 Aug 15;45(17):3569-72. [Content Brief]

[2]. Fiorucci S, et al. Protective effects of 6-ethyl chenodeoxycholic acid, a farnesoid X receptor ligand, in estrogen-induced cholestasis. J Pharmacol Exp Ther. 2005 May;313(2):604-12. [Content Brief]

[3]. Ghebremariam YT, et al. FXR agonist INT-747 upregulates DDAH expression and enhances sensitivity in high-salt fed Dahl rats. PLoS One. 2013 Apr 4;8(4):e60653. [Content Brief]

[4]. Verbeke L, et al. The FXR Agonist Obeticholic Acid Prevents Gut Barrier Dysfunction and Bacterial Translocation in Cholestatic Rats. Am J Pathol. 2015 Feb;185(2):409-19. [Content Brief]

Obeticholic acid 相关分类

Others

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

Ethanol / DMSO	1 mM	2.3774 mL	11.8869 mL	23.7739 mL	59.4347 mL
	5 mM	0.4755 mL	2.3774 mL	4.7548 mL	11.8869 mL
	10 mM	0.2377 mL	1.1887 mL	2.3774 mL	5.9435 mL
	15 mM	0.1585 mL	0.7925 mL	1.5849 mL	3.9623 mL
	20 mM	0.1189 mL	0.5943 mL	1.1887 mL	2.9717 mL
	25 mM	0.0951 mL	0.4755 mL	0.9510 mL	2.3774 mL
	30 mM	0.0792 mL	0.3962 mL	0.7925 mL	1.9812 mL
	40 mM	0.0594 mL	0.2972 mL	0.5943 mL	1.4859 mL
	50 mM	0.0475 mL	0.2377 mL	0.4755 mL	1.1887 mL
	60 mM	0.0396 mL	0.1981 mL	0.3962 mL	0.9906 mL
	80 mM	0.0297 mL	0.1486 mL	0.2972 mL	0.7429 mL
	100 mM	0.0238 mL	0.1189 mL	0.2377 mL	0.5943 mL

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Obeticholic acid (Synonyms: 奥贝胆酸; INT-747; 6-ECDCA; 6-Ethylchenodeoxycholic acid)

Customer Review

Other Forms of Obeticholic acid:

MCE 顾客使用本产品发表的 66 篇科研文献

Obeticholic acid 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

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纯度 & 产品资料

参考文献

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完整储备液配制表

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Obeticholic acid (Synonyms: 奥贝胆酸; INT-747; 6-ECDCA; 6-Ethylchenodeoxycholic acid)

Customer Review

Other Forms of Obeticholic acid:

Obeticholic acid 相关抗体

MCE 顾客使用本产品发表的 66 篇科研文献

Obeticholic acid 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

生物活性

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Obeticholic acid 相关抗体:

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完整储备液配制表

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