Obeticholic Acid (INT-747)

製品コードS7660 バッチS766006

印刷

化学情報

Synonyms

6-ECDCA, 6-Ethylchenodeoxycholic acid

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₆H₄₄O₄

分子量

420.63

CAS No.

459789-99-2

Solubility (25°C)*

体外

DMSO

84 mg/mL (199.7 mM)

Ethanol (warmed with 50ºC water bath)

84 mg/mL (199.7 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

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.
in vitro	In HuH7 cells, Obeticholic Acid (INT-747) acts as a potent FXR agonist with EC50 of 85 nM. ^[1]
in vivo	Obeticholic Acid (INT-747) promotes bile flow and protects hepatocytes against acute necrosis caused by LCA in a rat cholestasis model. ^[1] In WD-fed DBA mice, this compound (p.o.) improves proteinuria, ameliorates renal structural changes, and modulates renal inflammation and oxidative stress. ^[2] It (30 mg/kg p.o.) reactivates the FXR downstream signaling pathway and decreases portal pressure by lowering total IHVR without deleterious systemic hypotension in thioacetamide (TAA)-intoxicated and bile-duct-ligated (BDL) rats. ^[3]

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.

in vitro

In HuH7 cells, Obeticholic Acid (INT-747) acts as a potent FXR agonist with EC50 of 85 nM. ^[1]

in vivo

Obeticholic Acid (INT-747) promotes bile flow and protects hepatocytes against acute necrosis caused by LCA in a rat cholestasis model. ^[1]

In WD-fed DBA mice, this compound (p.o.) improves proteinuria, ameliorates renal structural changes, and modulates renal inflammation and oxidative stress. ^[2]

It (30 mg/kg p.o.) reactivates the FXR downstream signaling pathway and decreases portal pressure by lowering total IHVR without deleterious systemic hypotension in thioacetamide (TAA)-intoxicated and bile-duct-ligated (BDL) rats. ^[3]

プロトコル(参考用のみ)

キナーゼアッセイ	Binding Potency of Obeticholic Acid to FXR
キナーゼアッセイ	Obeticholic Acid (INT-747) 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.
細胞アッセイ	細胞株	HuH7 cells
	濃度	99 nM
	反応時間
	実験の流れ
動物実験	動物モデル	Rat cholestasis model
	投薬量	Saline
	投与方法	Infused at the right jugular vein using PE-50 polyethylene tubing

参考

https://pubmed.ncbi.nlm.nih.gov/12166927/
https://pubmed.ncbi.nlm.nih.gov/19776172/
https://pubmed.ncbi.nlm.nih.gov/24259407/

カスタマーフィードバック

: , , Integr Biol (Camb), 2017, 9(8):662-677

: Data from [Data independently produced by , , Cell Physiol Biochem, 2018, 48(1):158-172]

: Data from [Data independently produced by , , Toxicol Appl Pharmacol, 2017, 315:23-34]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Chenodeoxycholic acid modulates cholestatic niche through FXR/Myc/P-selectin axis in liver endothelial cells [ Nat Commun, 2025, 16(1):2093]	PubMed: 40025016
Inhibition of Farnesoid-x-receptor signaling during abdominal sepsis by dysbiosis exacerbates gut barrier dysfunction [ Cell Commun Signal, 2025, 23(1):236]	PubMed: 40399878
Dimethyl fumarate attenuates bile acid retention and liver fibrosis in a mouse model of cholestasis [ Am J Physiol Gastrointest Liver Physiol, 2025, 328(5):G558-G577]	PubMed: 40210415
Magneto-acoustic protein nanostructures for non-invasive imaging of tissue mechanics in vivo [ Nat Mater, 2024, 23(2):290-300]	PubMed: 37845321
FXR controls duodenogastric reflux-induced gastric inflammation through negatively regulating ER stress-associated TNXIP/NLPR3 inflammasome [ iScience, 2024, 27(3):109118]	PubMed: 38439955
Tetrahydropalmatine ameliorates hepatic steatosis in nonalcoholic fatty liver disease by switching lipid metabolism via AMPK-SREBP-1c-Sirt1 signaling axis [ Phytomedicine, 2023, 119:155005]	PubMed: 37562090
Ursodeoxycholic acid reduces antitumor immunosuppression by inducing CHIP-mediated TGF-β degradation [ Nat Commun, 2022, 13(1):3419]	PubMed: 35701426
Systemic ASBT inactivation protects against liver damage in obstructive cholestasis in mice [ JHEP Rep, 2022, 4-11:100573]	PubMed: 36160754
A Quantitative Systems Pharmacology Platform Reveals NAFLD Pathophysiological States and Targeting Strategies [ Metabolites, 2022, 12(6)528]	PubMed: 35736460
A Quantitative Systems Pharmacology Platform Reveals NAFLD Pathophysiological States and Targeting Strategies [ Metabolites, 2022, 10.3390/metabo12060528]	PubMed: 35736460

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。