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GW7647

Catalog No. T15453 CAS 265129-71-3

GW7647 is a potent agonist of PPARα (EC50s: 6 nM, 1.1 μM, and 6.2 μM for human PPARα, PPARγ, and PPARδ, respectively).

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GW7647, CAS 265129-71-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 45.00
5 mg	In stock	$ 101.00
10 mg	In stock	$ 150.00
25 mg	In stock	$ 256.00
50 mg	In stock	$ 441.00
100 mg	In stock	$ 636.00
1 mL * 10 mM (in DMSO)	In stock	$ 119.00

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Purity: 99.89%

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Description	GW7647 is a potent agonist of PPARα (EC50s: 6 nM, 1.1 μM, and 6.2 μM for human PPARα, PPARγ, and PPARδ, respectively).
Targets&IC50	PPARγ:1.1 μM (EC50)( Human PPARγ), PPARα:6 nM (EC50)( Human PPARα), PPARδ:6.2 μM (EC50)( Human PPARδ)
In vitro	GW7647 at a concentration of 50 nM, promotes PI3K and Akt (Ser473) phosphorylation, leading to an increase in NOS1 phosphorylation and subsequently elevating NO levels in stripped antral mucosa. Additionally, at the same concentration, it boosts the initial phase of Ca2+-mediated exocytotic events triggered by ACh in antral mucous cells, without independently inducing any exocytotic events. At a higher concentration of 1 μM, GW7647 substantially elevates PDZK1 protein levels to 129.7 ± 6.5% compared to controls in Caco2BBE cells, irrespective of IL-1β presence, and mitigates the IL-1β-induced reduction in PDZK1 expression. When combined with ACh, GW7647 augments the impact of wortmannin (50 nM) and AKT-inh (100 nM) on exocytotic activity in these cells. At 100 nM, GW7647 significantly decreases AQP9 protein levels by 43% in WIF-B9 hepatocytes and by 24% in HepG2 cells, though it shows no notable effects at 10 and 1,000 nM in WIF-B9 hepatocytes, nor does it significantly affect L-FABP protein levels in HepG2 hepatocytes.
In vivo	GW7647 (3 mg/kg per day) does not avoid the development of cardiac hypertrophy. It prevents the decline in left ventricular ejection fraction in vivo[4].

Molecular Weight	502.75
Formula	C29H46N2O3S
CAS No.	265129-71-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 60 mg/mL (119.34 mM)

References and Literature

1. Luo M, et al. IL-1β-Induced Downregulation of the Multifunctional PDZ Adaptor PDZK1 Is Attenuated by ERK Inhibition, RXRα, or PPARα Stimulation in Enterocytes. Front Physiol. 2017 Feb 7;8:61. 2. Tanaka S, et al. PPARα induced NOS1 phosphorylation via PI3K/Akt in guinea pig antral mucous cells: NO-enhancement in Ca(2+)-regulated exocytosis. Biomed Res. 2016;37(3):167-78. 3. Lebeck J, et al. Hepatic AQP9 expression in male rats is reduced in response to PPARα agonist treatment. Am J Physiol Gastrointest Liver Physiol. 2015 Feb 1;308(3):G198-205. 4. Lam VH, et al. Activating PPARα prevents post-ischemic contractile dysfunction in hypertrophied neonatal hearts. Circ Res. 2015 Jun 19;117(1):41-51. 5. Brown PJ, et al. Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis. Bioorg Med Chem Lett. 2001 May 7;11(9):1225-7.

Citations

1. Dou X, Huo T, Liu Y, et al.Discovery of novel and selective farnesoid X receptor antagonists through structure-based virtual screening, preliminary structure-activity relationship study, and biological evaluation.European Journal of Medicinal Chemistry.2024: 116323.

Related compound libraries

This product is contained In the following compound libraries：

Nuclear Receptor Compound Library Anti-Cancer Compound Library Glycometabolism Compound Library Anti-Diabetic Compound Library Mitochondria-Targeted Compound Library Anti-Obesity Compound Library Anti-Metabolism Disease Compound Library Bioactive Compounds Library Max Bioactive Compound Library Stem Cell Differentiation Compound Library

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Keywords

GW7647 265129-71-3 DNA Damage/DNA Repair Metabolism PPAR inhibit GW-7647 GW 7647 Peroxisome proliferator-activated receptors Inhibitor inhibitor

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