Obeticholic Acid | INT-747;6-ECDCA;Ocaliva.;6-Ethylchenodeoxycholic acid | Bile Acid | FXR

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奥贝胆酸 /Obeticholic Acid {[allProObj[0].p_purity_real_show]}

货号：A387805 同义名： INT-747;6-ECDCA

Obeticholic acid is a selective FXR agonist with EC50 of 99 nM and it has anticholestatic activity.

Obeticholic Acid 化学结构
CAS号：459789-99-2

Obeticholic Acid 3D分子结构
CAS号：459789-99-2

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Obeticholic Acid 纯度/质量文件产品仅供科研

货号：A387805 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JACS Au, 2024. Ambeed. [ A148168 ]; • JMC, 2024. Ambeed. [ A187643 ]; • JMC, 2024. Ambeed. [ A341145 , A633512 , A607865 , A167774 ]; • Biomacromolecules, 2024. Ambeed. [ A110759 ]; • Biomacromolecules, 2024. Ambeed. [ A203543 ]; 更多 >

Obeticholic Acid 生物活性

描述

The farnesoid X receptor (FXR) is an orphan member of the nuclear receptor superfamily that can be activated by small, lipophilic hormones. Obeticholic acid is a potent and selective FXR agonist with an EC₅₀ value of 99 nM. It also showed potent FXR agonist activity in HuH7 cells with an EC₅₀ value of 85 nM^[3]. The treatment of rat hepatocytes with 1 μM obeticholic acid increased mRNA expression of small heterodimer partner and bile salt export pump. The exposure to obeticholic acid also led to 70 - 80% reduction of cholesterol 7α-hydroxylase, oxysterol 12β-hydroxylase, and Na⁺/taurocholate cotransporting peptide in rat hepatocytes^[4]. The dosing of obeticholic acid at a rate of 3 µmol/kg/min completely reversed the impairment of bile flow and protected rats against lithocholic-induced liver cell injury^[3].

Obeticholic Acid 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
CHO cells		Function assay	5 h	Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay, EC50=0.755 μM	17685603
COS1 cells		Function assay		Agonist activity at FXR expressed in COS1 cells by cell-based bioluminescence assay, EC50=99 nM	20014870
HeLa cells		Function assay	24 h	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
human HepG2 cells	10 μM	Function assay	18 h	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

Obeticholic Acid 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02654236	Alcohol Consumption	Not Applicable	Recruiting	July 2019	United States, Indiana ... 展开 >> Indiana University Recruiting Indianapolis, Indiana, United States, 46202 Contact: Jennifer Lehman, RN 317-278-1872 jgeck@iu.edu Contact: Megan Comerford, BS, MPH 3172789226 mcomerfo@iu.edu Sub-Investigator: Naga Chalasani, MD Principal Investigator: Suthat Liangpunsakul, MD Sub-Investigator: David Crabb, MD 收起 <<
NCT00501592	Diabetes Mellitus, Type II ... 展开 >> Fatty Liver 收起 <<	Phase 2	Completed	-	United States, California ... 展开 >> Profil Institute for Clinical Research, Inc. Chula Vista, California, United States, 91911 UC San Diego VAMC San Diego, California, United States, 92161 United States, Texas Diabetes & Glandular Disease Research Associates, Inc. San Antonio, Texas, United States, 78229 United States, Virginia Virginia Commonwelath University Richmond, Virginia, United States, 23298 收起 <<
NCT00570765	Liver Cirrhosis, Biliary	Phase 2	Completed	-	United States, Michigan ... 展开 >> Henry Ford Novi, Michigan, United States, 39450 United States, Texas Baylor College of Medicine Houston, Texas, United States, 77030 United States, Virginia McGuire DVAMC Richmond, Virginia, United States, 23219 United States, Washington Virginia Mason Medical Center Seattle, Washington, United States, 98101 Austria Karls-Franzens University Graz, Austria, A8036 Canada, Alberta University of Alberta Edmonton, Alberta, Canada, T6G 2C8 Canada, Ontario University of Toronto Toronto, Ontario, Canada, M5T 2S8 Canada, Quebec Centre de Recherche du CHUM / University of Montreal Montreal, Quebec, Canada, H2X 1P1 France Hopital de l'Hotel Dieu Lyon, France, 69288 Hopital Saint-Antoine Paris, France, 75012 Germany Johann Wolfgang Goethe University Frankfurt, Germany, 60590 University Medical Centre Hamburg-Eppendorf Hamburg, Germany, D20246 Medical School of Hannover Hannover, Germany, 30623 University of Munich Munich, Germany, D81377 Spain Hospital Clinic i Provincial Barcelona, Spain, 08036 United Kingdom Queen Elizabeth Medical Center Edgbaston, Birmingham, United Kingdom, B15 2TH Royal Free Hospital Hampstead, London, United Kingdom, NW3 2QG John Radcliffe Hospital Headington, Oxford, United Kingdom, OX3 9DU Royal Infirmary Edinburgh, United Kingdom, EH16 4SA University Upon Tyne/Newcastle Newcastle Upon Tyne, United Kingdom, NE2 4HH 收起 <<

Obeticholic Acid 参考文献

[1]Verbeke L, Farre R, et al. Obeticholic acid, a farnesoid X receptor agonist, improves portal hypertension by two distinct pathways in cirrhotic rats. Hepatology. 2014 Jun;59(6):2286-98.

[2]Pellicciari R, Fiorucci S, 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.

[3]Pellicciari R, Fiorucci S, Camaioni E, et al. 6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity. J Med Chem. 2002;45(17):3569-3572. doi:10.1021/jm025529g

[4]Fiorucci S, Clerici C, Antonelli E, et al. Protective effects of 6-ethyl chenodeoxycholic acid, a farnesoid X receptor ligand, in estrogen-induced cholestasis. J Pharmacol Exp Ther. 2005;313(2):604-612. doi:10.1124/jpet.104.079665

Obeticholic Acid 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.38mL

0.48mL

0.24mL

11.89mL

2.38mL

1.19mL

23.77mL

4.75mL

2.38mL

Obeticholic Acid 技术信息

CAS号	459789-99-2
分子式	C₂₆H₄₄O₄
分子量	420.625

别名	INT-747;6-ECDCA;Ocaliva.;6-Ethylchenodeoxycholic acid
运输	蓝冰

存储条件

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(249.63 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 50 mg/mL(118.87 mM)，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇

动物实验配方

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT02654236	Alcohol Consumption	Not Applicable	Recruiting	July 2019	United States, Indiana ... 展开 >> Indiana University Recruiting Indianapolis, Indiana, United States, 46202 Contact: Jennifer Lehman, RN 317-278-1872 jgeck@iu.edu Contact: Megan Comerford, BS, MPH 3172789226 mcomerfo@iu.edu Sub-Investigator: Naga Chalasani, MD Principal Investigator: Suthat Liangpunsakul, MD Sub-Investigator: David Crabb, MD 收起 <<
NCT00501592	Diabetes Mellitus, Type II ... 展开 >> Fatty Liver 收起 <<	Phase 2	Completed	-	United States, California ... 展开 >> Profil Institute for Clinical Research, Inc. Chula Vista, California, United States, 91911 UC San Diego VAMC San Diego, California, United States, 92161 United States, Texas Diabetes & Glandular Disease Research Associates, Inc. San Antonio, Texas, United States, 78229 United States, Virginia Virginia Commonwelath University Richmond, Virginia, United States, 23298 收起 <<
NCT00570765	Liver Cirrhosis, Biliary	Phase 2	Completed	-	United States, Michigan ... 展开 >> Henry Ford Novi, Michigan, United States, 39450 United States, Texas Baylor College of Medicine Houston, Texas, United States, 77030 United States, Virginia McGuire DVAMC Richmond, Virginia, United States, 23219 United States, Washington Virginia Mason Medical Center Seattle, Washington, United States, 98101 Austria Karls-Franzens University Graz, Austria, A8036 Canada, Alberta University of Alberta Edmonton, Alberta, Canada, T6G 2C8 Canada, Ontario University of Toronto Toronto, Ontario, Canada, M5T 2S8 Canada, Quebec Centre de Recherche du CHUM / University of Montreal Montreal, Quebec, Canada, H2X 1P1 France Hopital de l'Hotel Dieu Lyon, France, 69288 Hopital Saint-Antoine Paris, France, 75012 Germany Johann Wolfgang Goethe University Frankfurt, Germany, 60590 University Medical Centre Hamburg-Eppendorf Hamburg, Germany, D20246 Medical School of Hannover Hannover, Germany, 30623 University of Munich Munich, Germany, D81377 Spain Hospital Clinic i Provincial Barcelona, Spain, 08036 United Kingdom Queen Elizabeth Medical Center Edgbaston, Birmingham, United Kingdom, B15 2TH Royal Free Hospital Hampstead, London, United Kingdom, NW3 2QG John Radcliffe Hospital Headington, Oxford, United Kingdom, OX3 9DU Royal Infirmary Edinburgh, United Kingdom, EH16 4SA University Upon Tyne/Newcastle Newcastle Upon Tyne, United Kingdom, NE2 4HH 收起 <<
NCT00501592	-		Completed	-	-
NCT00570765	-		Completed	-	-
NCT03633227	Liver Cirrhosis, Biliary	Phase 4	Recruiting	June 1, 2020	United States, California ... 展开 >> Inland Empire Liver Foundation Recruiting Rialto, California, United States, 92377 Contact: Darlene Romo 909-883-2999 dromo@ieliverfoundation.com Contact: Nazly Amaya 909-883-2999 namaya@ieliverfoundation.com Principal Investigator: Zeid Kayali, MD United States, Texas American Research Corporation at Texas Liver Institute Recruiting San Antonio, Texas, United States, 78215 Contact: Nicole Forsyth 210-253-3426 nforsyth@txliver.com Contact: Elisha Moreno 210-253-3426 emoreno@txliver.com Principal Investigator: Eric Lawitz, MD 收起 <<
NCT01914562	Healthy	Phase 1	Completed	-	United States, Arizona ... 展开 >> Celerion, Inc. Tempe, Arizona, United States, 85283 收起 <<
NCT03703076	-		Recruiting	April 2019	France ... 展开 >> Chu Grenoble Recruiting Grenoble, France, 38700 Contact: Vincent LEROY, MD 0476765450 ext +33 vleroy@chu-grenoble.fr Contact: Laure Bordy lbordy@chu-grenoble.fr Hopital Saint Antoine Recruiting Paris, France, 75571 Contact: Christophe Corpechot, MD 01 49 28 28 36 ext +33 christophe.corpechot@aphp.fr 收起 <<
NCT00550862	Liver Cirrhosis, Biliary	Phase 2	Completed	-	-
NCT00550862	-		Completed	-	-
NCT01473524	Primary Biliary Cirrhosis	Phase 3	Active, not recruiting	June 2018	-
NCT02177136	Primary Sclerosing Cholangitis... 展开 >> (PSC) 收起 <<	Phase 2	Completed	-	-
NCT01933503	Healthy	Phase 1	Completed	-	United States, Wisconsin ... 展开 >> Spaulding Clinical Research West Bend, Wisconsin, United States, 53095 收起 <<
NCT01904539	Hepatic Impairment	Phase 1	Completed	-	United States, Florida ... 展开 >> Clinical Pharmacology of Miami, Inc. Miami, Florida, United States, 33014 Orlando Clinical Research Center Orlando, Florida, United States, 32809 收起 <<
NCT03439254	Compensated Cirrhosis ... 展开 >> Nonalcoholic Steatohepatitis 收起 <<	Phase 3	Recruiting	July 2021	-
NCT03253276	Primary Biliary Cirrhosis	Early Phase 1	Recruiting	March 31, 2018	Denmark ... 展开 >> Susanne Keiding Recruiting Aarhus, Denmark, 8000 Contact: Susanne Keiding, prof +45 30939936 susakeid@rm.dk Contact: Michael Sørensen, PhD + 45 78463033 michsoer@rm.dk 收起 <<
NCT01865812	Primary Biliary Cirrhosis	Phase 2	Completed	-	United States, California ... 展开 >> Scripps Clinic La Jolla, California, United States, 92037 University of California, Davis Medical Center Sacramento, California, United States, 95817 United States, Florida University of Miami Miami, Florida, United States, 33136 United States, Indiana Indiana University Medical Center Indianapolis, Indiana, United States, 46202 United States, New York Beth Israel Medical Center New York, New York, United States, 10003 United States, Virginia McGuire DVAMC Richmond, Virginia, United States, 23249 United States, Washington Swedish Medical Center Seattle, Washington, United States, 98104 收起 <<
NCT01625026	Obesity Galls... 展开 >>tones 收起 <<	Phase 2	Completed	-	Sweden ... 展开 >> Hanns-Ulrich Marschall Göteborg, Sweden, 411 31 收起 <<
NCT02177136	-		Completed	-	-
NCT01265498	Nonalcoholic Fatty Liver Disea... 展开 >>se (NAFLD) Nonalcoholic Steatohepatitis (NASH) 收起 <<	Phase 2	Completed	-	United States, California ... 展开 >> University of California, San Diego San Diego, California, United States, 92103 University of California, San Francisco San Francisco, California, United States, 94143 United States, Indiana Indiana University Indianapolis, Indiana, United States, 46202 United States, Missouri St. Louis University Saint Louis, Missouri, United States, 63104 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Ohio Case Western Reserve University Cleveland, Ohio, United States, 44109 Cleveland Clinic Foundation Cleveland, Ohio, United States, 44195 United States, Virginia Virginia Commonwealth University Richmond, Virginia, United States, 23298 United States, Washington Virginia Mason Medical Center Seattle, Washington, United States, 98101 收起 <<
NCT01473524	-		Active, not recruiting	-	-
NCT02308111	Liver Cirrhosis, Biliary	Phase 4	Recruiting	April 2025	-
NCT02532335	Obesity	Phase 1	Recruiting	October 2019	Sweden ... 展开 >> Hanns-Ulrich Marschall Recruiting Göteborg, Sweden, 411 31 Contact: Hanns-Ulrich Marschall +4670774073 hanns-ulrich.marschall@gu.se Principal Investigator: Hanns-Ulrich Marschall, MD, PhD Sahlgrenska Academy Enrolling by invitation Göteborg, Sweden 收起 <<
NCT02039219	Alcoholic Hepatitis	Phase 2	Completed	-	United States, Indiana ... 展开 >> Indiana University Indianapolis, Indiana, United States, 46202 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 United States, Pennsylvania Einstein Healthcare Network Philadelphia, Pennsylvania, United States, 19141 United States, Virginia Virgina Commonwealth University Richmond, Virginia, United States, 23298 收起 <<
NCT01265498	-		Completed	-	-
NCT01865812	-		Completed	-	-
NCT02430077	Familial Partial Lipodystrophy	Phase 2	Recruiting	December 2019	United States, Texas ... 展开 >> UT Southwestern Medical Center 5323 Harry Hines Blvd Recruiting Dallas, Texas, United States, 75390-8537 Contact: Claudia Quittner, RN claudia.quittner@utsouthwestern.edu Contact: Chandna Vasandani, Ph.D 214-648-5074 chandna.vasandani@utsouthwestern.edu Principal Investigator: Abhimanyu Garg, MD Sub-Investigator: Zahid Ahmad, M.D. UT Southwestern Medical Center 5323 Harry Hines Blvd Recruiting Dallas, Texas, United States, 75390-8537 Principal Investigator: Abhimanyu Garg, MD Sub-Investigator: Zahid Ahmad, M.D. UT Southwestern Medical Center Recruiting Dallas, Texas, United States, 75390 Contact: Claudia Quittner, RN 214-648-9296 claudia.quittner@utsouthwestern.edu 收起 <<
NCT02633956	-		Completed	-	-
NCT01585025	Primary Bile Acid Malabsorptio... 展开 >>n Secondary Bile Acid Malabsorption Chronic Diarrhoea 收起 <<	Phase 2	Completed	-	United Kingdom ... 展开 >> Hammersmith Hospital, Imperial College Healthcare NHS Trust London, United Kingdom, W12 0HS Hammersmith Hospital London, United Kingdom, W12 0HS 收起 <<
NCT02548351	Non Alcoholic Steatohepatitis ... 展开 >>(NASH) 收起 <<	Phase 3	Recruiting	October 2022	-
NCT02633956	Nonalcoholic Steatohepatitis	Phase 2	Completed	-	United States, Arizona ... 展开 >> St. Joseph's Hospital and Medical Center Phoenix, Arizona, United States, 85013 United States, California Scripps Clinic La Jolla, California, United States, 92037 Inland Empire Liver Foundation Rialto, California, United States, 92377 United States, Florida Nature Coast Clinical Research Inverness, Florida, United States, 34452 University of Miamai, Schiff Center for Liver Diseases Miami, Florida, United States, 33136 South Florida Center of Gastroenterology Wellington, Florida, United States, 33414 Florida Medical Clinic, P.A. Zephyrhills, Florida, United States, 33542 United States, Hawaii The Queen's Medical Center - Liver Center Honolulu, Hawaii, United States, 96813 United States, Maryland Mercy Medical Center, Institute for Digestive Health & Liver Disease Baltimore, Maryland, United States, 21202 United States, Missouri Kansas City Research Institute Kansas City, Missouri, United States, 64131 St. Louis University Saint Louis, Missouri, United States, 63104 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 Cumberland Research Associates, LLC Fayetteville, North Carolina, United States, 28304 United States, Ohio Consultants for Clinical Research Cincinnati, Ohio, United States, 45249 United States, Pennsylvania Thomas Jefferson University Philadelphia, Pennsylvania, United States, 19107 United States, Rhode Island University Gastroenterology Liver Center Providence, Rhode Island, United States, 02905 United States, South Carolina Medical University of South Carolina Charleston, South Carolina, United States, 29425 United States, Tennessee ClinSearch Chattanooga, Tennessee, United States, 37421 United States, Texas Texas Clinical Research Institute, LLC Arlington, Texas, United States, 76012 Liver Associates of Texas, P.A. Houston, Texas, United States, 77030 American Research Corporation at the Texas Liver Institute San Antonio, Texas, United States, 78215 United States, Virginia McGuire DVAMC Richmond, Virginia, United States, 23249 收起 <<

奥贝胆酸 /Obeticholic Acid {[allProObj[0].p_purity_real_show]}

Obeticholic Acid 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Obeticholic Acid 质控信息

Obeticholic Acid 生物活性

Obeticholic Acid 细胞研究

Obeticholic Acid 临床研究

Obeticholic Acid 参考文献

Obeticholic Acid 实验方案

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奥贝胆酸 /Obeticholic Acid {[allProObj[0].p_purity_real_show]}

Obeticholic Acid 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Obeticholic Acid 质控信息

Obeticholic Acid 生物活性

Obeticholic Acid 细胞研究

Obeticholic Acid 临床研究

Obeticholic Acid 参考文献

Obeticholic Acid 实验方案

Obeticholic Acid 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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