Date published: 2025-10-30

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GW 4064 (CAS 278779-30-9)

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Alternate Names:
3-(2,6-Dichlorophenyl)-4-(3′-carboxy-2-chlorostilben-4-yl)oxymethyl-5-isopropylisoxazole
Application:
GW 4064 is a novel nonsteroidal FXR nuclear receptor activator
CAS Number:
278779-30-9
Purity:
≥98%
Molecular Weight:
542.84
Molecular Formula:
C28H22Cl3NO4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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GW 4064 is a selective, non-steroidal FXR (farnesoid X receptor) agonist (EC50 = 15 nM). GW 4064 displays no activity at other nuclear receptors at concentrations up to 1 μM. GW 4064 upregulates adipokine expression in preadipocytes and HepG2 cells. It can also reduce induction of proinflammatory cytokines by LPS in vitro.


GW 4064 (CAS 278779-30-9) References

  1. Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064.  |  Akwabi-Ameyaw, A., et al. 2008. Bioorg Med Chem Lett. 18: 4339-43. PMID: 18621523
  2. FXR agonist activity of conformationally constrained analogs of GW 4064.  |  Akwabi-Ameyaw, A., et al. 2009. Bioorg Med Chem Lett. 19: 4733-9. PMID: 19586769
  3. Synthetic FXR agonist GW4064 is a modulator of multiple G protein-coupled receptors.  |  Singh, N., et al. 2014. Mol Endocrinol. 28: 659-73. PMID: 24597548
  4. GW4064, a farnesoid X receptor agonist, upregulates adipokine expression in preadipocytes and HepG2 cells.  |  Xin, XM., et al. 2014. World J Gastroenterol. 20: 15727-35. PMID: 25400456
  5. GW4064 attenuates lipopolysaccharide‑induced hepatic inflammation and apoptosis through inhibition of the Toll‑like receptor 4‑mediated p38 mitogen‑activated protein kinase signaling pathway in mice.  |  Liu, HM., et al. 2018. Int J Mol Med. 41: 1455-1462. PMID: 29328388
  6. Farnesoid X Receptor Agonist GW4064 Inhibits Aromatase and ERβ Expression in Human Endometriotic Stromal Cells.  |  Wu, PL., et al. 2019. Reprod Sci. 26: 1111-1120. PMID: 30428773
  7. Bile acids promote gastric intestinal metaplasia by upregulating CDX2 and MUC2 expression via the FXR/NF-κB signalling pathway.  |  Yu, JH., et al. 2019. Int J Oncol. 54: 879-892. PMID: 30747230
  8. FXR agonist GW4064 improves liver and intestinal pathology and alters bile acid metabolism in rats undergoing small intestinal resection.  |  Cao, Y., et al. 2019. Am J Physiol Gastrointest Liver Physiol. 317: G108-G115. PMID: 30920307
  9. Suppressed farnesoid X receptor by iron overload in mice and humans potentiates iron-induced hepatotoxicity.  |  Xiong, H., et al. 2022. Hepatology. 76: 387-403. PMID: 34870866
  10. Bile acid homeostasis in female mice deficient in Cyp7a1 and Cyp27a1.  |  Rizzolo, D., et al. 2021. Acta Pharm Sin B. 11: 3847-3856. PMID: 35024311
  11. Farnesoid X receptor protects against cisplatin-induced acute kidney injury by regulating the transcription of ferroptosis-related genes.  |  Kim, DH., et al. 2022. Redox Biol. 54: 102382. PMID: 35767918
  12. GW4064 Alters Gut Microbiota Composition and Counteracts Autism-Associated Behaviors in BTBR T+tf/J Mice.  |  Liu, J., et al. 2022. Front Cell Infect Microbiol. 12: 911259. PMID: 35811667
  13. Effect of FXR agonist GW4064 in the treatment of hilar cholangiocarcinoma in rats.  |  Wang, JP., et al. 2022. Sci Rep. 12: 18873. PMID: 36344586

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

GW 4064, 5 mg

sc-218577
5 mg
$93.00