GW 7647A potent PPARα agonist with 200-fold selectivity over PPARγ and PPARδ

GW 7647 (CAS 265129-71-3)

GW 7647 | CAS 265129-71-3 is rated 5.0 out of 5 by 1.
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Synonym: 2-(4-(2-(1-Cyclohexanebutyl)-3-cyclohexylureido)ethyl)phenylthio)-2-methylpropionic acid; GW7647
Application: A potent PPARα agonist with 200-fold selectivity over PPARγ and PPARδ
CAS Number: 265129-71-3
Purity: >98%
Molecular Weight: 502.8
Molecular Formula: C29H46N2O3S
* Refer to Certificate of Analysis for lot specific data (including water content).
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GW 7647 is a potent PPARα agonist with 200-fold selectivity over PPARγ and PPARδ. This compound has also been found to cause an up-regulation of β-oxidation gene expression and an increase in palmitate oxidation. Additionally, glycolysis is strongly reduced at transcriptional levels by GW 7647 leading to a decrease in lactate and pyruvate production. Furthermore, this agent displays the ability to decrease glucose oxidation and inhibit lipogenesis and triglyceride esterification.


References

1. Brown, P.J., et al. 2001. Bioorg. Med. Chem. Lett. 11: 1225-1227. PMID: 11354382
2. Cunard, R., et al. 2002. J. Immunol. 168: 2795-2802. PMID: 11884448
3. Paukkeri, E.L., et al. 2007. Br. J. Pharmacol. 152: 1081-1091. PMID: 17891158
4. Ribet, C., et al. 2010. Endocrinology. 151: 123-133. PMID: 19887568

Physical State :
Solid
Solubility :
Soluble in DMSO (50 mg/ml), and ethanol (12 mg/ml). Insoluble in water.
Storage :
Store at room temperature
Boiling Point :
693.89° C at 760 mmHg (Predicted)
Density :
1.12 g/cm3 (Predicted)
Refractive Index :
n20D 1.57 (Predicted)
IC50 :
PPAR α: EC5050 = 1 nM (murine); PPAR α: EC5050 = 6 nM (human); PPAR γ: EC5050 = 1.1 µM (human); PPAR γ: EC5050 = 1.3 µM (murine); PPAR δ: EC5050 = 2.9 µM (murine); PPAR δ: EC5050 = 6.2 µM (human)
pK Values :
pKa: 3.79 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
UA2458293
PubChem CID :
3392731
MDL Number :
MFCD06798379
SMILES :
CC(C)(C(=O)O)SC1=CC=C(C=C1)CCN(CCCCC2CCCCC2)C(=O)NC3CCCCC3

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Certificate of Analysis

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GW 7647  Product Citations

See how others have used GW 7647. Click on the entry to view the PubMed entry .

Citations 1 to 3 of 3 total

PMID: # 25524540  Vergori, L. et al. 2015. Stem Cells. 33: 1292-303.

PMID: # 22234359  Ares-Carrasco S. et al. 2012. J Proteomics. 75(6): 1816-1829.

PMID: # 12118038  Muoio, DM. et al. 2002. J. Biol. Chem. 277: 26089-26097.

Citations 1 to 3 of 3 total
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Rated 5 out of 5 by from Lam Lam, VH. et al. (PubMed 25977309) investigated whether stimulating fatty acid -oxidation with GW7647, a peroxisome proliferator-activated receptor- (PPAR ) activator, would improve cardiac energy production and post-ischemic functional recovery in neonatal rabbit hearts subjected to volume overload-induced cardiac hypertrophy. Found that GW7647 treatment increased cardiac fatty acid -oxidation rates before and after ischemia, which resulted in a significant increase in overall ATP production and an improved in vitro post-ischemic functional recovery. -SCBT Publication Review
Date published: 2015-02-18
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