General description
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.
Biochem/physiol Actions
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
Packaging
Packaged under inert gas
Other Notes
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | white |
| solubility | ethanol: 12 mg/mL,DMSO: 50 mg/mL |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | S(C(C)(C)C(=O)O)c1ccc(cc1)CCN(CCCCC3CCCCC3)C(=O)NC2CCCCC2 |
| InChI | 1S/C29H46N2O3S/c1-29(2,27(32)33)35-26-18-16-24(17-19-26)20-22-31(28(34)30-25-14-7-4-8-15-25)21-10-9-13-23-11-5-3-6-12-23/h16-19,23,25H,3-15,20-22H2,1-2H3,(H,30,34)(H,32,33) |
| InChI key | PKNYXWMTHFMHKD-UHFFFAOYSA-N |
