Obeticholic Acid (INT-747)

別名：6-ECDCA, 6-Ethylchenodeoxycholic acid

製品コード：S7660 純度：99.77%

Obeticholic Acid (INT-747) is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Obeticholic Acid inhibits autophagy. Phase 3.

CAS No. 459789-99-2

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
25mg	JPY 59500	国内在庫あり
100mg	JPY 146500	国内在庫あり
1g	JPY 295500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（18）

カスタマーフィードバック3个实验数据

製品安全説明書

Obeticholic Acid (INT-747)関連製品

関連化合物ライブラリー	Metabolism Compound Library Anti-cancer Metabolism Compound Library Glutamine Metabolism Compound Library Carbohydrate Metabolism Compound Library Lipid Metabolism Compound Library	もっと見る

FXR阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
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
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生物活性

製品説明

Obeticholic Acid (INT-747) is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Obeticholic Acid inhibits autophagy. Phase 3.

Targets

FXR ^[1]

99 nM(EC50)

In Vitro
In vitro	In HuH7 cells, Obeticholic Acid acts as a potent FXR agonist with EC50 of 85 nM. ^[1]
Kinase Assay	Binding Potency of Obeticholic Acid to FXR
Kinase Assay	The compound is tested in an established cell-free ligand sensing assay, which measures the ligand-dependent recruitment of an SRC1 peptide to FXR by fluorescence resonance energy transfer.
実験結果図	Methods	Biomarkers	結果図	PMID
実験結果図	Western blot	XBP1s p-IRE1α		29377207

In Vivo
In Vivo	In rat cholestasis model, Obeticholic Acid promotes bile flow, and protects hepatocytes against acute necrosis caused by LCA. ^[1] Obeticholic Acid (p.o.) improves proteinuria, ameliorates renal structural changes, and modulates renal inflammation and oxidative stress in WD-fed DBA mice. ^[2] In thioacetamide (TAA)-intoxicated and bile-duct-ligated (BDL) rats, Obeticholic Acid (30 mg/kg p.o.) reactivates the FXR downstream signaling pathway and decreases portal pressure by lowering total IHVR without deleterious systemic hypotension. ^[3]
動物実験	動物モデル	Rat cholestasis model
	投与量	Saline
	投与経路	Infused at the right jugular vein using PE-50 polyethylene tubing

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
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
[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

化学情報

分子量	420.63	化学式	C₂₆H₄₄O₄
CAS No.	459789-99-2	SDF	Download Obeticholic Acid (INT-747) SDFをダウンロードする
Smiles	CCC1C2CC(CCC2(C3CCC4(C(C3C1O)CCC4C(C)CCC(=O)O)C)C)O
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 84 mg/mL ( (199.7 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 84 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

よくある質問（FAQ）

質問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):