Date published: 2025-12-1

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GW 590735 (CAS 622402-22-6)

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Application:
GW 590735 is a potent and selctive agonist of PPARα
CAS Number:
622402-22-6
Molecular Weight:
478.5
Molecular Formula:
C23H21F3N2O4S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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The peroxisome proliferator-activated receptors (PPARs) α, δ and γ are ligand-activated transcription factors that play a key role in lipid homeostasis. Activation of PPARα results in increased clearance of triglyceride (TG) rich very low-density lipoprotein (VLDL) via an upregulation of ApoA1, the principal lipoprotein component of HDL, and a reduction in plasma levels of ApoCIII (1). GW 590735 is a selective and potent agonist of PPARα with an EC50 value of 4 nM for the expression of a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARδ and PPARγ (1).


GW 590735 (CAS 622402-22-6) References

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  2. The treatment of dyslipidemia--what's left in the pipeline?  |  Rau, O., et al. 2008. ChemMedChem. 3: 206-21. PMID: 17963209
  3. Activation of peroxisome proliferator-activated receptor (PPAR)delta promotes reversal of multiple metabolic abnormalities, reduces oxidative stress, and increases fatty acid oxidation in moderately obese men.  |  Risérus, U., et al. 2008. Diabetes. 57: 332-9. PMID: 18024853
  4. PPAR-beta/delta agonists for Type 2 diabetes and dyslipidemia: an adopted orphan still looking for a home.  |  Billin, AN. 2008. Expert Opin Investig Drugs. 17: 1465-71. PMID: 18808307
  5. From molecular shape to potent bioactive agents II: fragment-based de novo design.  |  Proschak, E., et al. 2009. ChemMedChem. 4: 45-8. PMID: 19058280
  6. Circulating fibroblast growth factor 21 is induced by peroxisome proliferator-activated receptor agonists but not ketosis in man.  |  Christodoulides, C., et al. 2009. J Clin Endocrinol Metab. 94: 3594-601. PMID: 19531592
  7. Ligand-enhanced expression and in-cell assay of human peroxisome proliferator-activated receptor alpha ligand binding domain.  |  Velkov, T., et al. 2010. Protein Expr Purif. 70: 260-9. PMID: 19782138
  8. Selective CETP inhibition and PPARalpha agonism increase HDL cholesterol and reduce LDL cholesterol in human ApoB100/human CETP transgenic mice.  |  Hansen, MK., et al. 2010. J Cardiovasc Pharmacol Ther. 15: 196-202. PMID: 20332533
  9. Prediction of the PPARα agonism of fibrates by combined MM-docking approaches.  |  Lannutti, F., et al. 2011. J Mol Graph Model. 29: 865-75. PMID: 21414824
  10. Comparative Evaluation of Gemcabene and Peroxisome Proliferator-Activated Receptor Ligands in Transcriptional Assays of Peroxisome Proliferator-Activated Receptors: Implication for the Treatment of Hyperlipidemia and Cardiovascular Disease.  |  Bisgaier, CL., et al. 2018. J Cardiovasc Pharmacol. 72: 3-10. PMID: 29621036
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  12. Fenofibrate Reduces the Severity of Neuroretinopathy in a Type 2 Model of Diabetes without Inducing Peroxisome Proliferator-Activated Receptor Alpha-Dependent Retinal Gene Expression.  |  Enright, JM., et al. 2020. J Clin Med. 10: PMID: 33396512
  13. Restoring cellular NAD(P)H levels by PPARα and LXRα stimulation to improve mitochondrial complex I deficiency.  |  Frambach, SJCM., et al. 2022. Life Sci. 300: 120571. PMID: 35469913

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

GW 590735, 1 mg

sc-221701
1 mg
$66.00

GW 590735, 5 mg

sc-221701A
5 mg
$398.00