GW4064

製品コードS2782 バッチS278204

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C28H22Cl3NO4
分子量 542.84 CAS No. 278779-30-9
Solubility (25°C)* 体外 DMSO 100 mg/mL (184.21 mM)
Water Insoluble
Ethanol 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 GW4064 is an agonist of farnesoid X receptor (FXR) with EC50 of 65 nM in CV1 cell line and displays no activity at other nuclear receptors at concentrations up to 1 μM. GW4064 stimulates autophagy in MCF-7 cells.
in vitro

GW 4064 is a full agonist with EC50 values of 80 and 90 nM, respectively, in CV-1 cells transfected with mouse and human FXR expression vectors and an established reporter gene. There is no activity of GW 4064 on other nuclear receptors, including the retinoic acid receptor, at concentrations up to 1 μM. Thus, GW 4064 is a potent and selective nonsteroidal FXR agonist. [2]
in vivo

Pharmacokinetic analysis in rats shows that GW 4064 possesses an oral bioavailability of 10% with a t1/2 = 3.5 h. Fisher rats are dosed with GW 4064 by oral gavage. After 7 days, a dose-dependent lowering of serum triglycerides is observed in the rats receiving GW 4064, with an ED50 = 20 mg/kg. [2]

プロトコル(参考用のみ)

キナーゼアッセイ FXR Transient Transfection Assay
CV1 cells are maintained in DMEM high glucose medium. The CV1 cells are harvested 72 hours before transfection and plated in DMEM-F12 phenol red free medium containing 5% charcoal/dextran treated fetal bovine serum and 2 mM glutamine. On the day of transfection, the CV1 cells are harvested in DMEM-F12 phenol red free medium containing 5% charcoal/dextran treated fetal bovine serum and 2 mM glutamine, counted and seeded into a T-175 cm2 flask at a density of 14 million cells per flask before adding the transfection mix. The FuGENE® 6 transfection mix containing 0.55 μg pFA-CMV-GAL4-human FXR LBD expression plasmid, 10.92 μg of the (UAS)-tk-Luciferase reporter plasmid, 20.75 μg of pBluescript II KS+, and 3.82 μg of a human steroid receptor co-activator (SRC-1) construct is incubated and then added to the CV1 cells for overnight incubation in incubator. The transfected CV1 cells are harvested in DMEM-F12 phenol red free medium containing 5% charcoal/dextran treated fetal bovine serum and 2 mM glutamine. Transfected cells are added at a concentration of 3750 cells/well to 384-well plates containing ligands. Luciferase expression is measured using Steady-Glo?Luciferase Assay System 24 hr after incubation with ligand. GW4064X is used as the control, and data are normalized to GW4064X as % control.
細胞アッセイ 細胞株 HepG2 cells
濃度 10 µM
反応時間 2 h
実験の流れ

Cells were treated with indicated concentration of drug for 2 h.
動物実験 動物モデル Fisher rats
投薬量 0-100 mg/kg
投与方法 Orally, b.i.d.

カスタマーフィードバック

Data from [Data independently produced by , , Oncotarget, 2015, 6: 4226-38 ]

Data from [Data independently produced by , , Cardiovascular Research, 2018, doi: doi.org/10.1093/cvr/cvy093]

Data from [Data independently produced by , , RSC Adv, 2018, doi:10.1039/C8RA06345A]

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：

Farnesoid X receptor activation protects against renal fibrosis via modulation of β-catenin signaling [ Mol Metab, 2024, 79:101841] PubMed: 38036169
Ganoderma lucidum polysaccharide ameliorates cholesterol gallstone formation by modulating cholesterol and bile acid metabolism in an FXR-dependent manner [ Chin Med, 2024, 19(1):16] PubMed: 38268006
Resveratrol intervention attenuates chylomicron secretion via repressing intestinal FXR-induced expression of scavenger receptor SR-B1 [ Nat Commun, 2023, 14(1):2656] PubMed: 37160898
Insulin alleviates murine colitis through microbiome alterations and bile acid metabolism [ J Transl Med, 2023, 21(1):498] PubMed: 37491256
TMPRSS2 and SARS-CoV-2 SPIKE interaction assay for uHTS [ J Mol Cell Biol, 2023, 15(3)mjad017] PubMed: 36921991
Effects of perfluorooctanoic acid (PFOA) on gene expression profiles via nuclear receptors in HepaRG cells: Comparative study with in vitro transactivation assays [ Toxicology, 2023, 494:153577] PubMed: 37302725
Restraint stress promotes nonalcoholic steatohepatitis by regulating the farnesoid X receptor/NLRP3 signaling pathway [ Acta Biochim Biophys Sin (Shanghai), 2023, 55(12):1961-1971] PubMed: 37997375
Bile acid-sensitive tuft cells regulate biliary neutrophil influx [ Sci Immunol, 2022, 7(69):eabj1080] PubMed: 35245089
Intrahepatic Cholestasis of Pregnancy Increases Inflammatory Susceptibility in Neonatal Offspring by Modulating Gut Microbiota [ Front Immunol, 2022, 13:889646] PubMed: 35769469
Glycochenodeoxycholate Affects Iron Homeostasis via Up-Regulating Hepcidin Expression [ Nutrients, 2022, 14(15)3176] PubMed: 35956351

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