GW 4064 | Tocris Bioscience 2473 product information

product summary

company name :

Tocris Bioscience

product type :

chemical

product name :

GW 4064

catalog :

2473

quantity :

10 mg (also 50 mg)

price :

161 USD

more info or order :

Tocris Bioscience product webpage

citations: 17

Reference
Dong B, Singh A, Guo G, Young M, Liu J. Activation of FXR by obeticholic acid induces hepatic gene expression of SR-BI through a novel mechanism of transcriptional synergy with the nuclear receptor LXR. Int J Mol Med. 2019;43:1927-1938 pubmed publisher
Zhou H, Ni Z, Li T, Su L, Zhang L, Liu N, et al. Activation of FXR promotes intestinal metaplasia of gastric cells via SHP-dependent upregulation of the expression of CDX2. Oncol Lett. 2018;15:7617-7624 pubmed publisher
El Kasmi K, Vue P, Anderson A, Devereaux M, Ghosh S, Balasubramaniyan N, et al. Macrophage-derived IL-1β/NF-κB signaling mediates parenteral nutrition-associated cholestasis. Nat Commun. 2018;9:1393 pubmed publisher
Albrecht S, Fleck A, Kirchberg I, Hucke S, Liebmann M, Klotz L, et al. Activation of FXR pathway does not alter glial cell function. J Neuroinflammation. 2017;14:66 pubmed publisher
Kim H. The transcription cofactor CRTC1 protects from aberrant hepatic lipid accumulation. Sci Rep. 2016;6:37280 pubmed publisher
Verhaag E, Buist Homan M, Koehorst M, Groen A, Moshage H, Faber K. Hormesis in Cholestatic Liver Disease; Preconditioning with Low Bile Acid Concentrations Protects against Bile Acid-Induced Toxicity. PLoS ONE. 2016;11:e0149782 pubmed publisher
Gomez Ospina N, Potter C, Xiao R, Manickam K, Kim M, Kim K, et al. Mutations in the nuclear bile acid receptor FXR cause progressive familial intrahepatic cholestasis. Nat Commun. 2016;7:10713 pubmed publisher
Xin X, Zhong M, Yang G, Peng Y, Zhang Y, Zhu W. GW4064, a farnesoid X receptor agonist, upregulates adipokine expression in preadipocytes and HepG2 cells. World J Gastroenterol. 2014;20:15727-35 pubmed publisher
Lee J, Wagner M, Xiao R, Kim K, Feng D, Lazar M, et al. Nutrient-sensing nuclear receptors coordinate autophagy. Nature. 2014;516:112-5 pubmed publisher
Yang L, Broderick D, Jiang Y, Hsu V, Maier C. Conformational dynamics of human FXR-LBD ligand interactions studied by hydrogen/deuterium exchange mass spectrometry: insights into the antagonism of the hypolipidemic agent Z-guggulsterone. Biochim Biophys Acta. 2014;1844:1684-93 pubmed publisher
Hoeke M, Heegsma J, Hoekstra M, Moshage H, Faber K. Human FXR regulates SHP expression through direct binding to an LRH-1 binding site, independent of an IR-1 and LRH-1. PLoS ONE. 2014;9:e88011 pubmed publisher
Rondini E, Fang H, Runge Morris M, Kocarek T. Regulation of human cytosolic sulfotransferases 1C2 and 1C3 by nuclear signaling pathways in LS180 colorectal adenocarcinoma cells. Drug Metab Dispos. 2014;42:361-8 pubmed publisher
Kerr T, Matsumoto Y, Matsumoto H, Xie Y, Hirschberger L, Stipanuk M, et al. Cysteine sulfinic acid decarboxylase regulation: A role for farnesoid X receptor and small heterodimer partner in murine hepatic taurine metabolism. Hepatol Res. 2014;44:E218-28 pubmed publisher
Yu D, Lin W, Chen T, Forman B. Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discovery. Bioorg Med Chem. 2013;21:4266-78 pubmed publisher
Dai J, Wang H, Shi Y, Dong Y, Zhang Y, Wang J. Impact of bile acids on the growth of human cholangiocarcinoma via FXR. J Hematol Oncol. 2011;4:41 pubmed publisher
Fu D, Wakabayashi Y, Lippincott Schwartz J, Arias I. Bile acid stimulates hepatocyte polarization through a cAMP-Epac-MEK-LKB1-AMPK pathway. Proc Natl Acad Sci U S A. 2011;108:1403-8 pubmed publisher
Fickert P, Fuchsbichler A, Moustafa T, Wagner M, Zollner G, Halilbasic E, et al. Farnesoid X receptor critically determines the fibrotic response in mice but is expressed to a low extent in human hepatic stellate cells and periductal myofibroblasts. Am J Pathol. 2009;175:2392-405 pubmed publisher

product information

brand :

Tocris

master code :

2473

SKU :

2473/10

product name :

GW 4064

description :

Selective farnesoid X receptor (FXR) agonist

target :

LXR-like Receptor Agonists

category :

Small Molecules

unit size :

10 mg (also 50 mg)

purity :

97%

observed molecular weight :

542.84

url print :

?utm_source=distributor&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules

details of functionality :

Selective, non-steroidal farnesoid X receptor (FXR) agonist (EC50 = 15 nM). Displays no activity at other nuclear receptors at concentrations up to 1 u M. Improves hyperglycaemia and hyperlipidemia in diabetic db/db mice. Shown to suppress autophagy in nutrient-deprived mouse hepatocytes.

catalog number base :

2473

product keywords :

Selective farnesoid X receptor FXR agonists Receptors Liver LXR-like GW4064 GlaxoSmithKline GSK LXR-like Receptors Autophagy 2473,

extended description :

Selective farnesoid X receptor (FXR) agonist

chemical name text :

3-[2-[2-Chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]benzoic acid

formula :

C 28 H 22 Cl 3 NO 4

formula text :

C28H22Cl3NO4

cas num :

278779-30-9

2020 USD :

157

2021 USD :

161 USD

storage :

Store at +4°C

more info or order :

Tocris Bioscience product webpage