Obeticholic Acid (INT-747)

製品コードS7660 バッチS766004

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	84 mg/mL warmed with 50ºC water bath (199.7 mM)
		Water	Insoluble
* <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 acts as a potent FXR agonist with EC50 of 85 nM. ^[1]
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]

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 acts as a potent FXR agonist with EC50 of 85 nM. ^[1]

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]

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	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.
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

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：

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
Obeticholic Acid Inhibits Anxiety via Alleviating Gut Microbiota-Mediated Microglia Accumulation in the Brain of High-Fat High-Sugar Diet Mice [ Nutrients, 2021, 13(3)940]	PubMed: 33803974
Resolution of NASH and Hepatic Fibrosis by the GLP-1R/GcgR Dual-Agonist Cotadutide via Modulating Mitochondrial Function and Lipogenesis [ Nat Metab, 2020, 2(5):413-431]	PubMed: 32478287
Stimulation of soluble guanylate cyclase exerts antiinflammatory actions in the liver through a VASP/NF-κB/NLRP3 inflammasome circuit [ Proc Natl Acad Sci U S A, 2020, 117(45):28263-28274]	PubMed: 33106416
FXR Regulates Intestinal Cancer Stem Cell Proliferation [Fu T, et al Cell, 2019, 176(5):1098-1112]	PubMed: 30794774

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。

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