GW 4064
Based on 56 publication(s) in Google Scholar
GW 4064 is a potent FXR agonist with an EC50 of 65 nM.
For research use only. We do not sell to patients.
- Purity: 99.79%
- CAS No.: 278779-30-9
- Formula: C28H22Cl3NO4
- Molecular Weight:542.84
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) GW 4064
More- Cell Host Microbe. 2024 Feb 14;32(2):191-208.e9. [Abstract]
- Nat Commun. 2023 Mar 9;14(1):1305. [Abstract]
- Cell Death Differ. 2026 Mar 11. [Abstract]
- Acta Pharm Sin B. 2019 May;9(3):526-536. [Abstract]
- Adv Sci (Weinh). 2025 Oct 27:e15370. [Abstract]
- Adv Sci (Weinh). 2024 Dec 31:e2412071. [Abstract]
- Theranostics. 2022 Aug 15;12(14):6130-6142. [Abstract]
- Microbiome. 2025 Feb 4;13(1):36. [Abstract]
- Microbiome. 2024 Feb 5;12(1):20. [Abstract]
- Environ Sci Technol. 2026 Mar 31;60(12):8958-8970. [Abstract]
- Gut Microbes. 2025 Dec 31;17(1):2582944. [Abstract]
- EBioMedicine. 2018 Nov:37:322-333. [Abstract]
- Research (Wash D C). 2022 Nov 2:2022:9784081. [Abstract]
- Pharmacol Res. 2025 Apr 25:107738. [Abstract]
- J Am Soc Nephrol. 2019 Jun;30(6):962-978. [Abstract]
- J Pharm Anal. 2021 Feb;11(1):122-127. [Abstract]
- Dev Cell. 2019 Feb 25;48(4):460-474.e9. [Abstract]
- Sci Total Environ. 2023 Apr 15:869:161701. [Abstract]
- J Transl Med. 2019 Dec 13;17(1):418. [Abstract]
- Cell Mol Gastroenterol Hepatol. 2024 Aug 21:101392. [Abstract]
- Cell Rep. 2021 Jul 20;36(3):109398. [Abstract]
- J Med Chem. 2025 Oct 15. [Abstract]
- J Med Chem. 2025 Jun 12;68(11):11127-11148. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Phytother Res. 2025 Aug 20. [Abstract]
- Oncoimmunology. 2023 May 25;12(1):2217024. [Abstract]
- J Agric Food Chem. 2023 Oct 4;71(39):14365-14378. [Abstract]
- Ecotoxicol Environ Saf. 2024 Nov 5:287:117266. [Abstract]
- Hepatol Int. 2024 Jun;18(3):1040-1052. [Abstract]
- JCI Insight. 2020 Dec 8;6(1):e141640. [Abstract]
- Eur J Med Chem. 2025 Jan 15:286:117284. [Abstract]
- Chem Biol Interact. 2024 Feb 1:389:110869. [Abstract]
- Commun Biol. 2025 Jul 5;8(1):1009. [Abstract]
- Commun Biol. 2022 Jul 28;5(1):750. [Abstract]
- Int J Mol Sci. 2018 Jun 28;19(7). pii: E1898. [Abstract]
- Biomolecules. 2025 Jun 28;15(7):943. [Abstract]
- Eur J Pharmacol. 2025 Feb 1:177329. [Abstract]
- FASEB J. 2026 Mar 31;40(6):e71667. [Abstract]
- FEBS J. 2025 Feb 11. [Abstract]
- FASEB J. 2022 Apr;36(4):e22243. [Abstract]
- FASEB J. 2019 Feb;33(2):2472-2483. [Abstract]
- Nutr Metab. 2022 Aug 23;19(1):57. [Abstract]
- iScience. 2021 Aug 19;24(9):103003. [Abstract]
- J Biol Chem. 2024 Sep 12:107765. [Abstract]
- Aquaculture. 2021, 736248.
- Brain Behav Immun Health. 2024 Sep 4:41:100856. [Abstract]
- Phytochemistry. 2023 Feb:206:113550. [Abstract]
- FEBS Lett. 2017 Sep;591(18):2836-2847. [Abstract]
- Immun Inflamm Dis. 2025 Apr;13(4):e70155. [Abstract]
- J Mol Histol. 2025 Jul 31;56(4):243. [Abstract]
- Biotechnol Lett. 2020 Aug;42(8):1327-1336. [Abstract]
- Am J Transl Res. 2021 Aug 15;13(8):9296-9305. [Abstract]
- bioRxiv. 2024 July 06.
- bioRxiv. 2024 Feb 18:2024.02.16.580658. [Abstract]
- Research Square Preprint. 2023 Oct 28.
- Patent. US20200368199A1.
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RT-PCR
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Biological Activity
EC50: 65 nM (FXR)[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CV-1 | EC50 |
65 nM
Compound: 1a, GW-4064
|
Agonist activity at FXR expressed in african green monkey CV1 cells by luciferase reporter transient transfection assay
Agonist activity at FXR expressed in african green monkey CV1 cells by luciferase reporter transient transfection assay
|
[PMID: 18621523] |
| CV-1 | EC50 |
65 nM
Compound: 1a, GW-4064
|
Agonist activity at human FXR transfected in african green monkey CV1 cells by luciferase reporter gene transient transfection assay
Agonist activity at human FXR transfected in african green monkey CV1 cells by luciferase reporter gene transient transfection assay
|
[PMID: 19410460] |
| CV-1 | EC50 |
65 nM
Compound: 1, GW-4064
|
Increase in human FXR-mediated transient transcription of luciferase reporter gene transfected in african green monkey CV1 cells
Increase in human FXR-mediated transient transcription of luciferase reporter gene transfected in african green monkey CV1 cells
|
[PMID: 19586769] |
| CV-1 | EC50 |
65 nM
Compound: 1a, GW-4064
|
Agonist activity at human FXR LBD iexpressed in monkey CV-1 cells assessed as transactivation of luciferase reporter gene expression
Agonist activity at human FXR LBD iexpressed in monkey CV-1 cells assessed as transactivation of luciferase reporter gene expression
|
[PMID: 21256005] |
| CV-1 | EC50 |
65 nM
Compound: 1a, GW-4064
|
Agonist activity at human FXR LBD transfected in african green monkey CV1 cells after overnight incubation by luciferase reporter gene assay
Agonist activity at human FXR LBD transfected in african green monkey CV1 cells after overnight incubation by luciferase reporter gene assay
|
[PMID: 21890356] |
| CV-1 | EC50 |
65 nM
Compound: GW4064
|
Agonist activity at FXR (unknown origin) transfected into african green monkey CV1 cells assessed as ligand-mediated transcription by luciferase reporter/ transient transfection assay
Agonist activity at FXR (unknown origin) transfected into african green monkey CV1 cells assessed as ligand-mediated transcription by luciferase reporter/ transient transfection assay
|
[PMID: 25499883] |
| HEK293 | EC50 |
0.07 μM
Compound: GW-4064
|
Agonistic activity at FXR in HEK293 cells by GAL4 transactivation activity
Agonistic activity at FXR in HEK293 cells by GAL4 transactivation activity
|
[PMID: 17292610] |
| HEK293 | EC50 |
30 nM
Compound: GW-4064
|
Agonist activity at human full length FXR transfected in HEK293 cells coexpressing pTRexDest/pGL2promotor assessed as luciferase activity by direct reporter cellular assay
Agonist activity at human full length FXR transfected in HEK293 cells coexpressing pTRexDest/pGL2promotor assessed as luciferase activity by direct reporter cellular assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
35 nM
Compound: GW-4064
|
Agonist activity at human GST-fused FXR LBD expressed in HEK293 cells coexpressing GAL4-DNA bindig domain and pFRluc by mammalian one-hybrid assay
Agonist activity at human GST-fused FXR LBD expressed in HEK293 cells coexpressing GAL4-DNA bindig domain and pFRluc by mammalian one-hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
0.07 μM
Compound: 1, GW4064
|
Agonist activity at human recombinant FXR expressed in HEK293 cells coexpressing CMX-GAL4N by luciferase reporter gene assay
Agonist activity at human recombinant FXR expressed in HEK293 cells coexpressing CMX-GAL4N by luciferase reporter gene assay
|
[PMID: 22583617] |
| HEK293 | EC50 |
26 nM
Compound: GW4064
|
Agonist activity at human FXR expressed in HEK293 cells by luciferase reporter gene assay
Agonist activity at human FXR expressed in HEK293 cells by luciferase reporter gene assay
|
[PMID: 25305688] |
| HEK293 | EC50 |
373 nM
Compound: GW4064
|
Agonist activity at human FXR transfected in HEK293 cells assessed as transcriptional activity by luciferase reporter gene assay
Agonist activity at human FXR transfected in HEK293 cells assessed as transcriptional activity by luciferase reporter gene assay
|
[PMID: 26568144] |
| HEK293 | EC50 |
35 nM
Compound: 1; GW4064
|
Agonist activity at C-terminal Gal4-tagged human FXR (187 to 472 residues) expressed in HEK-293 cells co-expressing pFRluc by mammalian one hybrid assay
Agonist activity at C-terminal Gal4-tagged human FXR (187 to 472 residues) expressed in HEK-293 cells co-expressing pFRluc by mammalian one hybrid assay
|
[PMID: 27268696] |
| HEK-293T | EC50 |
95 nM
Compound: 2; GW4064
|
Agonist activity at human FXR expressed in HEK293T cells assessed as BSEP promoter driven cellular transcriptional activity after 24 hrs by luciferase reporter gene assay
Agonist activity at human FXR expressed in HEK293T cells assessed as BSEP promoter driven cellular transcriptional activity after 24 hrs by luciferase reporter gene assay
|
[PMID: 29148806] |
| HEK-293T | IC50 |
>10000 nM
Compound: 1; GW4064
|
Antagonist activity at human VDR transfected in HEK293T cells measured after 24 hrs by luciferase reporter gene assay
Antagonist activity at human VDR transfected in HEK293T cells measured after 24 hrs by luciferase reporter gene assay
|
[PMID: 32616182] |
| HEK-293T | EC50 |
0.09 μM
Compound: 3; GW4064
|
Activation of human FXR LBD expressed in HEK293T cells assessed as induction of receptor activation incubated for 12 to 14 hrs by luciferase reporter gene assay
Activation of human FXR LBD expressed in HEK293T cells assessed as induction of receptor activation incubated for 12 to 14 hrs by luciferase reporter gene assay
|
[PMID: 32687365] |
| HEK-293T | EC50 |
0.61 μM
Compound: 4; GW4064
|
Agonist activity at human farnesoid-X-receptor expressed in HEK293T cells co-expressing human RXRalpha assessed as receptor activation after 20 hrs by dual luciferase reporter assay
Agonist activity at human farnesoid-X-receptor expressed in HEK293T cells co-expressing human RXRalpha assessed as receptor activation after 20 hrs by dual luciferase reporter assay
|
10.1039/C5MD00149H |
| HeLa | EC50 |
0.51 μM
Compound: 3, GW4064
|
Agonist activity at human full length FXR expressed in HeLa cells cotransfected with pSG5-human RXR after 24 hrs by Dual-Glo luciferase reporter gene assay
Agonist activity at human full length FXR expressed in HeLa cells cotransfected with pSG5-human RXR after 24 hrs by Dual-Glo luciferase reporter gene assay
|
[PMID: 25934227] |
| HepG2 | EC50 |
0.02 μM
Compound: 3; GW4064
|
Transactivation of human FXR (unknown origin) expressed in HepG2 cells co-expressing pSG5RXR/pGL4.70 after 24 hrs post transfection by luciferase reporter gene assay
Transactivation of human FXR (unknown origin) expressed in HepG2 cells co-expressing pSG5RXR/pGL4.70 after 24 hrs post transfection by luciferase reporter gene assay
|
[PMID: 30996771] |
| HT-29 | IC50 |
13.8 μM
Compound: 74; GW4064
|
Antiproliferative activity against human HT-29 cells incubated for 48 hrs by CCK-8 method
Antiproliferative activity against human HT-29 cells incubated for 48 hrs by CCK-8 method
|
[PMID: 38142509] |
| Huh-7 | EC50 |
13.2 nM
Compound: 1; GW4064
|
Agonist activity at human FXR expressed in human HuH7 cells by luciferase reporter gene assay
Agonist activity at human FXR expressed in human HuH7 cells by luciferase reporter gene assay
|
[PMID: 32616182] |
| SW-620 | IC50 |
7.6 μM
Compound: 74; GW4064
|
Antiproliferative activity against human SW620 cells incubated for 48 hrs by CCK-8 method
Antiproliferative activity against human SW620 cells incubated for 48 hrs by CCK-8 method
|
[PMID: 38142509] |
Treatment with different concentrations of GW4064 (1, 2.5, 5, 10 μM) reduces the lipid accumulation in the cells. Concordantly, GW4064 treatment significantly represses oleic acid-induced CD36 protein levels in a dose-dependent manner. Taken together, these data indicate that prevention of hepatic lipid accumulation is likely due to an inhibition of Cd36 expression by long-term GW4064 treatment[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 278779-30-9
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Appearance Solid
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Molecular Weight 542.84
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Formula C28H22Cl3NO4
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Color White to off-white
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SMILES
O=C(C1=CC=CC(/C=C/C2=CC=C(C=C2Cl)OCC3=C(ON=C3C4=C(Cl)C=CC=C4Cl)C(C)C)=C1)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (56)
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Journal Impact Factor
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Most Recent
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Cell Host Microbe
A gut microbiota-bile acid axis promotes intestinal homeostasis upon aspirin-mediated damage. [Abstract]2024 Feb 14;32(2):191-208.e9. PMID: 38237593 -
Nat Commun
Gut microbiota alters host bile acid metabolism to contribute to intrahepatic cholestasis of pregnancy. [Abstract]2023 Mar 9;14(1):1305. PMID: 36894566 -
Cell Death Differ
Gut-derived hyodeoxycholate reprograms the spleen-eye immunometabolic axis to suppress autoimmune uveitis. [Abstract]2026 Mar 11. PMID: 41813862 -
Acta Pharm Sin B
2019 May;9(3):526-536. PMID: 31193776 -
Adv Sci (Weinh)
Medicago Sativa L. Saponin-Driven Lactobacillus Intestinalis Restores Intestinal Stemness in Naturally Aged Mice via the Bile Acid-FXR-Wnt Signaling Axis. [Abstract]2025 Oct 27:e15370. PMID: 41144719 -
Adv Sci (Weinh)
Gut Microbiota-Derived Hyocholic Acid Enhances Type 3 Immunity and Protects Against Salmonella enterica Serovar Typhimurium in Neonatal Rats. [Abstract]2024 Dec 31:e2412071. PMID: 39737849 -
Theranostics
Lgr5 + cell fate regulation by coordination of metabolic nuclear receptors during liver repair. [Abstract]2022 Aug 15;12(14):6130-6142. PMID: 36168631 -
Microbiome
Microbiota governs host chenodeoxycholic acid glucuronidation to ameliorate bile acid disorder induced diarrhea. [Abstract]2025 Feb 4;13(1):36. PMID: 39905483 -
Microbiome
2024 Feb 5;12(1):20. PMID: 38317217 -
Environ Sci Technol
Microcystin-LR Disrupts Bile Acid Homeostasis, Driving Cholestatic Liver Injury and Gallstones via FXR/SHP Antagonism. [Abstract]2026 Mar 31;60(12):8958-8970. PMID: 41837707 -
Gut Microbes
Antibiotic cocktail-induced changes in gut microbiota drive alteration of bile acid metabolism to restrain Th17 differentiation through the FXR-NLRP3 axis. [Abstract]2025 Dec 31;17(1):2582944. PMID: 41305918 -
EBioMedicine
Noncanonical farnesoid X receptor signaling inhibits apoptosis and impedes liver fibrosis. [Abstract]2018 Nov:37:322-333. PMID: 30337250 -
Research (Wash D C)
Activation of Pancreatic Acinar FXR Protects against Pancreatitis via Osgin1-Mediated Restoration of Efficient Autophagy. [Abstract]2022 Nov 2:2022:9784081. PMID: 36405253 -
Pharmacol Res
FXR as a pivotal role linking JNK and G0s2 mitigates triptolide-induced hepatotoxicity through the regulation of metabolic disorder of liver. [Abstract]2025 Apr 25:107738. PMID: 40288593 -
J Am Soc Nephrol
Protein O-GlcNAcylation Is Essential for the Maintenance of Renal Energy Homeostasis and Function via Lipolysis during Fasting and Diabetes. [Abstract]2019 Jun;30(6):962-978. PMID: 31043434 -
J Pharm Anal
2021 Feb;11(1):122-127. PMID: 33717618 -
Dev Cell
FGF15 Activates Hippo Signaling to Suppress Bile Acid Metabolism and Liver Tumorigenesis. [Abstract]2019 Feb 25;48(4):460-474.e9. PMID: 30745141 -
Sci Total Environ
Binding, activity and risk assessment of bisphenols toward farnesoid X receptor pathway: In vitro and in silico study. [Abstract]2023 Apr 15:869:161701. PMID: 36709907 -
J Transl Med
FXR activation alleviates tacrolimus-induced post-transplant diabetes mellitus by regulating renal gluconeogenesis and glucose uptake. [Abstract]2019 Dec 13;17(1):418. PMID: 31836014
GW 4064 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2019 Dec 13;17(1):418. [Abstract]
FXR suppresses gluconeogenesis and enhances glucose uptake in the HK-2 cell lines. The protein expression of FXR is obviously upregulates by GW4064 at 24, 48 and 72 h in the HK-2 cell lines.
GW 4064 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2019 Dec 13;17(1):418. [Abstract]
FXR suppresses gluconeogenesis and enhances glucose uptake in the HK-2 cell lines. GW4064 at 4 μM inhibits the mRNA level of FXR.
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Cell Mol Gastroenterol Hepatol
2024 Aug 21:101392. PMID: 39179177 -
Cell Rep
Neuronal activity recruits the CRTC1/CREB axis to drive transcription-dependent autophagy for maintaining late-phase LTD. [Abstract]2021 Jul 20;36(3):109398. PMID: 34289350 -
J Med Chem
Discovery of the First-In-Class HSD17B13/PPAR Multitarget Modulators for the Treatment of Metabolic Dysfunction-Associated Steatohepatitis. [Abstract]2025 Oct 15. PMID: 41088966 -
J Med Chem
Discovery of Highly Potent, Selective, and Liver-Targeting HSD17B13 Inhibitor with Robust In Vivo Anti-MASH Activity. [Abstract]2025 Jun 12;68(11):11127-11148. PMID: 40387207 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Phytother Res
Monosaccharide and Disaccharide Saponins of Shade-Dried Gynostemma Pentaphyllum Confer Metabolic Benefits in Mice With Non-Alcoholic Fatty Liver Disease. [Abstract]2025 Aug 20. PMID: 40833710 -
Oncoimmunology
2023 May 25;12(1):2217024. PMID: 37261088 -
J Agric Food Chem
Farnesoid X Receptor Plays a Key Role in Ochratoxin A-Induced Nephrotoxicity by Targeting Ferroptosis In Vivo and In Vitro. [Abstract]2023 Oct 4;71(39):14365-14378. PMID: 37750412 -
Ecotoxicol Environ Saf
Aristolochic acid-induced dyslipidemia and hepatotoxicity: The potential role of FXR and AHR receptors. [Abstract]2024 Nov 5:287:117266. PMID: 39509784 -
Hepatol Int
Bile acids induce liver fibrosis through the NLRP3 inflammasome pathway and the mechanism of FXR inhibition of NLRP3 activation. [Abstract]2024 Jun;18(3):1040-1052. PMID: 38172440 -
JCI Insight
BRD4 inhibition and FXR activation, individually beneficial in cholestasis, are antagonistic in combination. [Abstract]2020 Dec 8;6(1):e141640. PMID: 33290278 -
Eur J Med Chem
Design, synthesis, and biological evaluation of imidazolidinone derivatives as potent PPARα/δ agonists for the treatment of cholestatic liver diseases. [Abstract]2025 Jan 15:286:117284. PMID: 39827490 -
Chem Biol Interact
GW4064 inhibits migration and invasion through cathepsin B and MMP2 downregulation in human bladder cancer. [Abstract]2024 Feb 1:389:110869. PMID: 38216027 -
Commun Biol
Ursodeoxycholic acid alleviates aortic aneurysm and dissection through the intestinal farnesoid X receptor/ceramide synthase 2 axis. [Abstract]2025 Jul 5;8(1):1009. PMID: 40617906 -
Commun Biol
2022 Jul 28;5(1):750. PMID: 35902736 -
Int J Mol Sci
Farnesoid X Receptor Activation Enhances Transforming Growth Factor β-Induced Epithelial-Mesenchymal Transition in Hepatocellular Carcinoma Cells. [Abstract]2018 Jun 28;19(7). pii: E1898. PMID: 29958417
GW 4064 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2018 Jun 28;19(7). pii: E1898. [Abstract]
Western blotting for p-FAK and total FAK. Cells are treated with vehicle control (Cont), 10 μM GW4064, or 32 μM GS in the absence or presence of 10 ng/mL TGF-β for 48 h. .
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Biomolecules
Significant Reduction of Chenodeoxycholic Acid and Glycochenodeoxycholic Acid in the Elderly with Severe COVID-19. [Abstract]2025 Jun 28;15(7):943. PMID: 40723815 -
Eur J Pharmacol
GW4064 inhibits migration and invasion in human glioblastoma multiforme through the downregulation of PKCα. [Abstract]2025 Feb 1:177329. PMID: 39900326 -
FASEB J
Dysbiosis in the Gut-Liver Axis Is Associated With Low Bone Mass During Murine Cholestasis. [Abstract]2026 Mar 31;40(6):e71667. PMID: 41801071 -
FEBS J
FXR suppress Müller cell activation by regulating cGAS/STING pathway in diabetic retinopathy. [Abstract]2025 Feb 11. PMID: 39932043 -
FASEB J
Farnesoid X receptor agonist attenuates subchondral bone osteoclast fusion and osteochondral pathologies of osteoarthritis via suppressing JNK1/2/NFATc1 pathway. [Abstract]2022 Apr;36(4):e22243. PMID: 35224782 -
FASEB J
Farnesoid X receptor-α is a proviral host factor for hepatitis B virus that is inhibited by ligands in vitro and in vivo. [Abstract]2019 Feb;33(2):2472-2483. PMID: 30307769
GW 4064 purchased from MedChemExpress. Usage Cited in: FASEB J. 2019 Feb;33(2):2472-2483. [Abstract]
FXRa protein expression in nontransduced (treated with DMSO or GW4064 for 9 d) and transduced shFXRa-dHepaRG cells, by Western blot analysis.
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Nutr Metab
Alpha-linolenic acid inhibits hepatocellular carcinoma cell growth through Farnesoid X receptor/β-catenin signaling pathway. [Abstract]2022 Aug 23;19(1):57. PMID: 35999582 -
iScience
Metabolic nuclear receptors coordinate energy metabolism to regulate Sox9+ hepatocyte fate. [Abstract]2021 Aug 19;24(9):103003. PMID: 34505013 -
J Biol Chem
PPARγ and C/EBPα enable adipocyte differentiation upon inhibition of histone methyltransferase PRC2 in malignant tumors. [Abstract]2024 Sep 12:107765. PMID: 39276936 -
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Brain Behav Immun Health
Dried bear bile exerts its antidepressant effect by modulating adrenal FXR to reduce peripheral glucocorticoid levels. [Abstract]2024 Sep 4:41:100856. PMID: 39290473 -
Phytochemistry
Coumaronochromones, flavanones, and isoflavones from the twigs and leaves of Erythrina subumbrans inhibit PTP1B and nitric oxide production. [Abstract]2023 Feb:206:113550. PMID: 36481312 -
FEBS Lett
A rapid administration of GW4064 inhibits the NLRP3 inflammasome activation independent of farnesoid X receptor agonism. [Abstract]2017 Sep;591(18):2836-2847. PMID: 28787755
GW 4064 purchased from MedChemExpress. Usage Cited in: FEBS Lett. 2017 Sep;591(18):2836-2847. [Abstract]
GW4064 inhibits NLRP3 inflammasome activation. The human PBMCs are primed with 500 ng/mL LPS for 3 h followed by GW4064 of indicated concentration(s) and different second signal stimulations, including Nigericin. The protein levels of activated caspase-1 and cleaved IL-1b are detected by western blot.
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Immun Inflamm Dis
Farnesoid X Receptor Regulated Sepsis-Induced Abnormal Bile Acid Metabolism via the Fibroblast Growth Factor 15/Fibroblast Growth Factor Receptor 4 Pathway. [Abstract]2025 Apr;13(4):e70155. PMID: 40192065 -
J Mol Histol
Nuclear receptor FXR inhibits ferroptosis to alleviate hepatic ischemia-reperfusion injury by targeting GPX4 in a mouse model. [Abstract]2025 Jul 31;56(4):243. PMID: 40742574 -
Biotechnol Lett
Transcriptional regulation of microRNA-126a by farnesoid X receptor in vitro and in vivo. [Abstract]2020 Aug;42(8):1327-1336. PMID: 32221722 -
Am J Transl Res
Effect of Glycyrrhiza uralensis against ulcerative colitis through regulating the signaling pathway of FXR/P-gp. [Abstract]2021 Aug 15;13(8):9296-9305. PMID: 34540046 -
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bioRxiv
2024 Feb 18:2024.02.16.580658. PMID: 38405928 -
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Solvent & Solubility
DMSO : 100 mg/mL (184.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
DMF : 100 mg/mL (184.22 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMF 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 5 mg/mL (9.21 mM); Suspended solution; Need ultrasonic
Add each solvent one by one: 0.5% CMC/saline water
Solubility: 5 mg/mL (9.21 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Mouse liver cells (BNL CL.2) are maintained in a humidified incubator under 5% CO2 at 37°C in Dulbecco's Modified Eagle's Medium (DMEM). When cells are divided into six-well plates and reach ~90% confluence, sub-confluent cells are washed three times with phosphate buffered saline (PBS) and replaced with serum-free DMEM supplemented with 1% fatty acid-free BSA. Oleic acid (final concentration 500 μM) and GW4064 at various concentrations are added and incubated for 24 h. Cells are then fixed with 4% formaldehyde for Oil Red O staining or harvested for protein and western blot analysis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
Fifteen-week-old male C57BL/6 mice are fed a high-fat diet with or without additional 0.2% Cholesterol and received twice weekly injections of GW 4064 (50 mg/kg, intra-peritoneal) or carrier solution (DMSO) solution for 6 weeks. Animals are weighed weekly and their body composition is determined using EchoMRI-100TM from Echo Medical Systems.
Rats[3]
Animals. Adult male CRL:CD(SD)IGS rats weighing 300-350 g, are used. Twenty-four hours after laparotomy, groups of rats (n=6) receive intraperitoneal injections once daily for 4 days. Bile duct-ligated (BDL) rats are treated with 5 mL/kg corn oil as vehicle, 30 mg/kg GW4064 in corn oil, or 15 mg/kg TUDCA in corn oil. Sham-operated animals received 5 mL/kg corn oil vehicle. Four hours after the final dose, serum and livers are collected for analysis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Akwabi-Ameyaw A, et al.Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064. Bioorg Med Chem Lett, 2008, 18(15), 4339-4343. [Content Brief]
[2]. Ma Y, et al. Synthetic FXR agonist GW4064 prevents diet-induced hepatic steatosis and resistance. Pharm Res. 2013 May;30(5):1447-57. [Content Brief]
[3]. Liu Y, et al. Hepatoprotection by the farnesoid X receptor agonist GW4064 in rat models of intra- and extrahepatic cholestasis. J Clin Invest. 2003 Dec;112(11):1678-87. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / DMF | 1 mM | 1.8422 mL | 9.2108 mL | 18.4216 mL | 46.0541 mL |
| 5 mM | 0.3684 mL | 1.8422 mL | 3.6843 mL | 9.2108 mL | |
| 10 mM | 0.1842 mL | 0.9211 mL | 1.8422 mL | 4.6054 mL | |
| 15 mM | 0.1228 mL | 0.6141 mL | 1.2281 mL | 3.0703 mL | |
| 20 mM | 0.0921 mL | 0.4605 mL | 0.9211 mL | 2.3027 mL | |
| 25 mM | 0.0737 mL | 0.3684 mL | 0.7369 mL | 1.8422 mL | |
| 30 mM | 0.0614 mL | 0.3070 mL | 0.6141 mL | 1.5351 mL | |
| 40 mM | 0.0461 mL | 0.2303 mL | 0.4605 mL | 1.1514 mL | |
| 50 mM | 0.0368 mL | 0.1842 mL | 0.3684 mL | 0.9211 mL | |
| 60 mM | 0.0307 mL | 0.1535 mL | 0.3070 mL | 0.7676 mL | |
| 80 mM | 0.0230 mL | 0.1151 mL | 0.2303 mL | 0.5757 mL | |
| 100 mM | 0.0184 mL | 0.0921 mL | 0.1842 mL | 0.4605 mL |