Obeticholic Acid (INT-747)
别名: 6-ECDCA, 6-Ethylchenodeoxycholic acid 中文名称：奥贝胆酸
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
客户使用Selleck的Obeticholic Acid (INT-747)发表文献18篇
客户使用该产品的3个实验数据
产品质控
Obeticholic Acid (INT-747)相关产品
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FXR抑制剂选择性比较
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 |
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| 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] |
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|---|---|---|---|---|
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | XBP1s p-IRE1α |
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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] |
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|---|---|---|
| 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 |
|---|---|---|---|---|---|
| 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 |
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) | |||
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体外溶解度 |
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 Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 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
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）
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）
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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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"
