GW7647

A cell-permeable urea-substituted thioisobutyric acid (ureido-TiBA) compound that acts as a potent and selective PPARα agonist (PPARα, γ and δ - EC₅₀ = 6 nM, 1.1 µM and 6.2 µM for human; 1 nM, 1.3 µM and 2.9 µM for murine, respectively). Also displays in vivo lipid-lowering activity in rats.

A cell-permeable, urea-substituted, thioisobutyric acid (ureido-TiBA) compound that acts as a potent and selective peroxisome proliferator-activated receptor α (PPARα) agonist (EC₅₀ = 6 nM for human PPARα, 1.1 µM for human PPARγ, and 6.2 µM human PPARδ; 1 nM for murine PPARα, 1.3 µM for murine PPARγ, and 2.9 µM murine PPARδ). Also shown to lower lipid levels in rats.

Cell permeable: yes

EC50 = 6 nM, 1.1 µM and 6.2 µM for human PPARα, γ and δ, respectively; EC50 = 1 nM, 1.3 µM and 2.9 µM for murine PPARα, γ and δ, respectively

Primary Target
PPARα

Product does not compete with ATP.

Reversible: no

Packaged under inert gas

Toxicity: Irritant (B)

Muoio, D.M., et al. 2002. J. Biol. Chem.277, 26089.
Brown, P.J., et al. 2001. Bioorg. Med. Chem. Lett.11, 1225.
Oliver, W.R. Jr., et al. 2001. Proc. Natl. Acad. Sci. USA98, 5306.
Poirier, H., et al. 2001. Biochem. J.355, 481.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany