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Chemical Structure| 278779-30-9 Chemical Structure| 278779-30-9

Structure of GW 4064
CAS No.: 278779-30-9

Chemical Structure| 278779-30-9

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GW 4064 is an FXR agonist with an IC50 of 190 nM. GW 4064 regulates cholesterol and lipid metabolism and is mainly used in research on metabolic diseases and liver disorders.

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Product Details of GW 4064

CAS No. :278779-30-9
Formula : C28H22Cl3NO4
M.W : 542.84
SMILES Code : O=C(O)C1=CC=CC(/C=C/C2=CC=C(OCC3=C(C(C)C)ON=C3C4=C(Cl)C=CC=C4Cl)C=C2Cl)=C1
MDL No. :MFCD09971006
InChI Key :BYTNEISLBIENSA-MDZDMXLPSA-N
Pubchem ID :9893571

Safety of GW 4064

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H319-H413
Precautionary Statements:P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Hepa1c1c7 cells 100 nM 6 hours To test whether FXR directly inhibits autophagy, results showed that GW4064 treatment attenuated autophagy PMC4257899
primary mouse hepatocytes (PMH) 0.5 μM 10 minutes To detect Tyr phosphorylation levels of FXR, results showed that GW4064 treatment did not significantly increase Tyr phosphorylation of FXR. PMC6030054
Neonatal rat ventricular myocytes (NRVMs) 3-5 μmol/L 24 hours GW 4064 significantly reduced cell viability and induced apoptosis in NRVMs PMC3689100
Caco-2 cells 100 μM To validate the inhibition of FXR by Gly-MCA PMC4682112
Primary human hepatocytes 1 µM 12 or 48 hours To evaluate the effect of GW4064 on the expression of MDR3, BSEP, and SHP genes in primary human hepatocytes. Results showed that GW4064 significantly induced the expression of MDR3, BSEP, and SHP. PMC281645
mouse hepatocytes 2 μM 24 hours induced Abcg5/g8 mRNA expression PMC3079544
primary human hepatocytes 2 μM 24 hours induced ABCG5/G8 mRNA and protein expression PMC3079544

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Xenograft tumor model Intraperitoneal injection 100 mg/kg Every other day for 20 days GW4064 significantly inhibited tumor growth, and the inhibitory effect was even more pronounced when combined with CDCA. PMC3207959
Mice LPS-induced sepsis model Intraperitoneal injection 100 mg/kg Twice a week for 4 weeks GW 4064 failed to improve survival, serum IL-1β levels, and activation of caspase 1/IL-1β in PMs in LPS-induced septic mice. PMC6624427
Nude mice Xenograft tumor model Intraperitoneal injection 30 mg/kg GW4064 significantly inhibited tumor growth, and the inhibitory effect was even more pronounced when used in combination with CDCA. PMC3207959
C57BL/6 mice FXR knockout mice intraperitoneal injection 5 mg/kg Single dose, lasting 6 hours To test the inhibitory effect of GW4064 on autophagy, results showed that GW4064 treatment reduced the number of autophagic vesicles and decreased LC3-II levels PMC4257899
Mice C57BL/6 mice Tail vein injection 30 mg/kg 7 days To investigate the effect of miR-144 overexpression on ABCA1 protein levels and plasma HDL cholesterol levels, results showed that overexpression of miR-144 significantly reduced ABCA1 protein levels and plasma HDL cholesterol levels. PMC3995747
mice high-fat diet-induced obesity model oral 30 mg/kg Single dose, lasting 6 hours To validate the reversal of Gly-MCA action by GW4064 PMC4682112
Rats Bile duct ligation model and α-naphthylisothiocyanate (ANIT)-induced cholestasis model Intraperitoneal injection 5 days To evaluate the hepatoprotective effects of GW4064 in bile duct ligation and ANIT-induced cholestasis models. Results showed that GW4064 significantly reduced serum ALT, AST, and LDH levels, decreased liver necrosis and inflammatory cell infiltration, and induced the expression of bile acid transporters. PMC281645

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.84mL

0.37mL

0.18mL

9.21mL

1.84mL

0.92mL

18.42mL

3.68mL

1.84mL

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