GW-7647 is a potent, selective agonist of human and murine PPARα4 It activates human PPARα, PPARγ, and PPARδ with EC50 values of 0.006, 1.1 and 6.2 µM, respectively.
Chemical Formula: C29H46N2O3S
Exact Mass: 502.3229
Molecular Weight: 502.76
Elemental Analysis: C, 69.28; H, 9.22; N, 5.57; O, 9.55; S, 6.38
Appearance: White to off-white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
GW7647 (1 μM) causes a significant increase of PDZK1 protein expression to 129.7 ± 6.5% of vehicle treated control in Caco2BBE cells in the absence and presence of IL-1β. GW7647 also attenuates the IL-1β-mediated decrease in PDZK1 expression. GW7647 (50 nM) stimulates the PI3K phosphorylation followed by the Akt (Ser473) phosphorylation, which induces NOS1 phosphorylation increased the amounts of NO released in the stripped antral mucosa. GW7647 (50 nM) enhances the initial phase of Ca2+-regulated exocytotic events stimulated by ACh in antral mucous cells, but GW7647 alone does not evoke any exocytotic event. GW7647 plus ACh stimulates the effects of wortmannin (50 nM) and AKT-inh (100 nM) on the exocytotic events in antral mucous cells. GW 7647 (100 nM) reduces the AQP9 protein abundance by 43%, but it shows not significant effect at 10 and 1,000 nM in WIF-B9 hepatocytes. GW 7647 (100 nM) causes a 24% reduction in AQP9 protein abundance in HepG2 cells, however, it does not significantly increase the protein abundance of L-FABP in HepG2 hepatocytes.
GW7647 (3 mg/kg per day) does not prevent the development of cardiac hypertrophy, but it prevents the decline in left ventricular ejection fraction in vivo.
- Strömqvist M, Olsson JA, Kärrman A, Brunström B. Transcription of genes involved in fat metabolism in chicken embryos exposed to the peroxisome proliferator-activated receptor alpha (PPARα) agonist GW7647 or to perfluorooctane sulfonate (PFOS) or perfluorooctanoic acid (PFOA). Comp Biochem Physiol C Toxicol Pharmacol. 2012 Jun;156(1):29-36. doi: 10.1016/j.cbpc.2012.03.004. PubMed PMID: 22465071.
- van der Krieken SE, Popeijus HE, Konings M, Dullens SP, Mensink RP, Plat J. C/EBP-β Is Differentially Affected by PPARα Agonists Fenofibric Acid and GW7647, But Does Not Change Apolipoprotein A-I Production During ER-Stress and Inflammation. J Cell Biochem. 2016 Sep 12. doi: 10.1002/jcb.25731. [Epub ahead of print] PubMed PMID: 27618583.
- Zhang H, Gao Y, Qiao PF, Zhao FL, Yan Y. PPAR-α agonist regulates amyloid-β generation via inhibiting BACE-1 activity in human neuroblastoma SH-SY5Y cells transfected with APPswe gene. Mol Cell Biochem. 2015 Oct;408(1-2):37-46. doi: 10.1007/s11010-015-2480-5. PubMed PMID: 26092426.
- Ham J, Cho SJ, Ko J, Chin J, Kang H. A facile one-pot preparation of alkyl aminoaryl sulfides for the synthesis of GW7647 as an agonist of peroxisome proliferator-activated receptor alpha. J Org Chem. 2006 Jul 21;71(15):5781-4. PubMed PMID: 16839165.
- Russo R, LoVerme J, La Rana G, D'Agostino G, Sasso O, Calignano A, Piomelli D. Synergistic antinociception by the cannabinoid receptor agonist anandamide and the PPAR-alpha receptor agonist GW7647. Eur J Pharmacol. 2007 Jul 2;566(1-3):117-9. PubMed PMID: 17434479; PubMed Central PMCID: PMC1997313.
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