Obeticholic Acid (INT-747)

别名: 6-ECDCA, 6-Ethylchenodeoxycholic acid 中文名称：奥贝胆酸

目录号：S7660 Purity: 99.72%

Obeticholic Acid (INT-747)是一种有效的选择性farnesoid X receptor (FXR)兴奋剂，EC50为99 nM。Obeticholic Acid 可抑制自噬。Phase 3。

Obeticholic Acid (INT-747) Chemical Structure

CAS: 459789-99-2

规格	价格	库存
10mM (1mL in DMSO)	1203.93	现货
5mg	809.97	现货
25mg	2851.57	现货
100mg	8001.23	现货
1g	16134.3	现货
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产品质控

批次：纯度： 99.72%

99.72

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细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
HepG2	Function assay	10 uM	18 hrs	Agonist activity at FXR in human HepG2 cells assessed as upregulation of OST-alpha mRNA expression at 10 uM after 18 hrs by RT-PCR analysis	24387325
HepG2	Function assay	10 uM	18 hrs	Agonist activity at FXR in human HepG2 cells assessed as upregulation of SHP mRNA expression at 10 uM after 18 hrs by RT-PCR analysis	24387325
HepG2	Function assay	10 uM	18 hrs	Agonist activity at FXR in human HepG2 cells assessed as upregulation of BESP mRNA expression at 10 uM after 18 hrs by RT-PCR analysis	24387325
HepG2	Function assay	20 uM		Induction of FXR-mediated SHP mRNA expression in human HepG2 cells at 20 uM by RT-PCR	21459580
HepG2	Function assay	1 uM		Induction of FXR-mediated SHP mRNA expression in human HepG2 cells at 1 uM by RT-PCR	21459580
HepG2	Function assay	20 uM		Induction of FXR-mediated BSEP mRNA expression in human HepG2 cells at 20 uM by RT-PCR	21459580
HepG2	Function assay	20 uM		Induction of FXR-mediated Ostbeta mRNA expression in human HepG2 cells at 20 uM by RT-PCR	21459580
HepG2	Function assay	1 uM		Induction of FXR-mediated down-regulation of Cyp7A1 mRNA expression in human HepG2 cells at 1 uM by RT-PCR	21459580
HepG2	Function assay	20 uM		Induction of FXR-mediated down-regulation of Cyp7A1 mRNA expression in human HepG2 cells at 20 uM by RT-PCR	21459580
HepG2	Function assay	20 uM		Agonist activity at human FXR expressed in HepG2 cells assessed as renilla luciferase activity at 20 uM by luciferase based transactivation assay	21459580
HepG2	Function assay	1 uM		Induction of FXR-mediated BSEP mRNA expression in human HepG2 cells at 1 uM by RT-PCR	21459580
HepG2	Function assay	1 uM		Induction of FXR-mediated Ostbeta mRNA expression in human HepG2 cells at 1 uM by RT-PCR	21459580
HepG2	Function assay	10 uM		Transactivation of human FXR transfected in human HepG2 cells at 10 uM by beta-galactosidase reporter gene assay	24387325
HeLa	Function assay		24 hrs	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, EC50 = 0.16 μM.	25934227
HEK293T	Function assay		24 hrs	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, EC50 = 0.042 μM.	29148806
insect cells	Function assay		1 hr	Agonist activity at recombinant human GST-tagged FXR ligand binding domain (193 to 472 residues) expressed in baculovirus infected insect cells assessed as induction of interaction with biotin labelled SRC-1 after 1 hr by HTRF assay, EC50 = 0.01 μM.	29148806
insect cells	Function assay		1 hr	Agonist activity at recombinant human GST-tagged FXR LBD (193 to 472 residues) expressed in baculovirus-infected insect cells assessed as recruitment of biotinylated SRC1 peptide measured after 1 hr by Alphascreen assay, EC50 = 0.18 μM.	29259742
COS1	Function assay		5 hrs	Agonist activity at human FXR expressed in COS1 cells after 5 hrs by CRE-driven luciferase reporter gene assay, EC50 = 0.361 μM.	17685603
CHO	Function assay		5 hrs	Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay, EC50 = 0.755 μM.	17685603
HEK293	Function assay		1 hr	Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assay, EC50 = 0.84 μM.	29259742
COS1	Function assay			Agonist activity at FXR expressed in COS1 cells by cell-based bioluminescence assay, EC50 = 0.099 μM.	20014870
HeLa	Function assay			Agonist activity at human FXR expressed in human HeLa cells assessed as receptor activation by BSEP promoter-driven firefly luciferase reporter gene assay, EC50 = 0.16 μM.	25255039
NCI-H716	Function assay			Agonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assay, EC50 = 20 μM.	21459580
GLUTag	Function assay			Agonist activity at GP-BAR1 in mouse GLUTag cells assessed as increase in intracellular cAMP level	24387325
GLUTag	Function assay			Agonist activity at GP-BAR1 in mouse GLUTag cells assessed as increase in GLP-1 release	24387325
点击查看更多细胞系数据

生物活性

产品描述

Obeticholic Acid (INT-747)是一种有效的选择性farnesoid X receptor (FXR)兴奋剂，EC50为99 nM。Obeticholic Acid 可抑制自噬。Phase 3。

靶点

FXR ^[1]

99 nM(EC50)

体外研究(In Vitro)
体外研究活性	在HuH7细胞中，Obeticholic Acid是一种有效的FXR激动剂，EC50 为85 nM。^[1]
实验图片	检测方法	检测指标	实验图片	PMID
实验图片	Western blot	XBP1s p-IRE1α		29377207

体内研究(In Vivo)
体内研究活性	在大鼠胆汁郁积模型中，Obeticholic Acid促进胆汁流动，并保护肝细胞免受LCA引起的急性坏死。^[1] 在WD喂养的DBA 小鼠体内，Obeticholic Acid (p.o.)改善蛋白尿和肾脏结构的改变，并调节肾脏炎症和氧化应激。^[2] 在硫代乙酰胺(TAA)中毒的和胆小管结扎的(BDL)大鼠体内，Obeticholic Acid (30 mg/kg p.o.) 通过降低总IHVR，恢复FXR下游信号通路，并降低门静脉压力，而不产生有害的全身性低血压。^[3]
动物实验	Animal Models	大鼠胆汁郁积模型
	Dosages	生理盐水
	Administration	使用 PE-50 聚乙烯管在右颈动脉进行注射

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05740631	Recruiting	Healthy	Universitaire Ziekenhuizen KU Leuven\|Intercept Pharmaceuticals	August 22 2022	Not Applicable
NCT02633956	Completed	Nonalcoholic Steatohepatitis	Intercept Pharmaceuticals	December 4 2015	Phase 2
NCT02548351	Terminated	Non Alcoholic Steatohepatitis (NASH)	Intercept Pharmaceuticals	September 22 2015	Phase 3

参考文献
[1] Pellicciari R, et al. J Med Chem. 2002, 45(17), 3569-3572. [2] Wang XX, et al. Am J Physiol Renal Physiol. 2009, 297(6), F1587-1596. [3] Verbeke L, et al. Hepatology. 2014, 59(6), 2286-2298.

参考文献

化学信息&溶解度

分子量	420.63	分子式	C₂₆H₄₄O₄
CAS号	459789-99-2	SDF	Download Obeticholic Acid (INT-747) SDF
Smiles	CCC1C2CC(CCC2(C3CCC4(C(C3C1O)CCC4C(C)CCC(=O)O)C)C)O
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 84 mg/mL ( (199.7 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 84 mg/mL (199.7 mM)

Water : Insoluble

DMSO : 84 mg/mL ( (199.7 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 84 mg/mL (199.7 mM)

Water : Insoluble

DMSO : 84 mg/mL ( (199.7 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 84 mg/mL (199.7 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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操作手册

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常见问题及建议解决方法

问题 1:
What formulation can we use to dissolve Obeticholic Acid (Catalog No.S7660) for mice in vivo study?

回答：
You can use the vehicle of: 1% wt/vol methyl-cellulose as indicated in this paper, http://www.sciencedirect.com/science/article/pii/S0925443911000883 "daily oral gavage with 5 mg/kg/day INT-747 (6-ethyl-chenodeoxycholic acid, Obeticholic acid, Intercept Pharmaceuticals Inc, New York, NY) or vehicle (1% wt/vol methyl-cellulose) from 3 days prior to induction of colitis"

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):