General description
A cell-permeable phenoxyacetic acid derivative that acts as a potent and selective peroxisome proliferator activator receptor δ (PPARδ) agonist (Ki = 6 nM for hPPAR δ and 730 nM for hPPARγ). Induces adipocyte differentiation in NIH-PPARδ cells at 500 nM. Also reported to raise total cholesterol in insulin-resistant db/db mice without altering glucose or triglyceride levels. Shown to increase uncoupling protein 3 (UCP3) gene expression in L6 myotubes. Also shown to inhibit cytokine-induced expression of vascular cell adhesion molecule-1 (VCAM-1) and the secretion of monocyte chemotactic protein-1 (MCP-1) in Eahy926 cells.
A cell-permeable phenoxyacetic acid derivative that acts as a potent and selective peroxisome proliferator activator receptor δ (PPARδ) agonist (Ki = 6 nM for hPPARδ and 730 nM for hPPARγ). Potently induces adipocyte differentiation in NIH-PPARδ cells at 500 nM and raises total cholesterol in insulin resistant db/db mice without altering glucose or triglycerides levels. Increases UCP3 (uncoupling protein 3) gene expression in L6 myotubes. Inhibits cytokine-induced expression of VCAM-1 (vascular cell adhesion molecule-1) and the secretion of MCP-1 (monocyte chemotactic protein-1) in EAhy926 cells.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Peroxisome proliferator activator receptor δ (PPAR@delta;)
Product does not compete with ATP.
Reversible: no
Target Ki: 6 nM for hPPARδ and 730 nM for hPPARγ
Packaging
Packaged under inert gas
Warning
Toxicity: Irritant (B)
Reconstitution
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Rival, Y., et al. 2002. Eur. J. Pharmacol.435, 143.
Castrillo, A., et al. 2001. J. Biol. Chem.276, 34082.
Hansen, J.B., et al. 2001. J. Biol. Chem.276, 3175.
Son, C., et al. 2001. Endocrinology142, 4189.
Wilkie, N., et al. 2001. J. Neurochem.78, 1135.
Leibowitz, M.D., et al. 2000. FEBS Lett.473, 333.
Berger, J., et al. 1999. J. Biol. Chem.274, 6718.
Lim, H., et al. 1999. Genes Dev.13, 1561.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 41141931
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 422175-5MG