422175

L-165,041

A cell-permeable phenoxyacetic acid derivative that acts as a potent and selective peroxisome proliferator activator receptor δ (PPARδ) agonist (K_i = 6 nM for hPPARδ and 730 nM for hPPARγ).

• Sinônimo(s): L-165,041, Compound P, L165041, 4-[3-(2-Propyl-3-hydroxy-4-acetyl)phenoxy]propyloxyphenoxy-acetic acid, PPAR Agonist VIII, PPARα Agonist III, PPARγ Agonist VII
• Fórmula empírica (Notação de Hill): C₂₂H₂₆O₇
• Número CAS: 79558-09-1
• Peso molecular: 402.44
• Número MDL: MFCD04974501
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥98% (HPLC)
• forma: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: white
• solubilidade: 1 M NaOH: 40 mg/mL; DMSO: 5 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: 2-8°C
• InChI: 1S/C22H26O7/c1-3-5-19-20(11-10-18(15(2)23)22(19)26)28-13-4-12-27-16-6-8-17(9-7-16)29-14-21(24)25/h6-11,26H,3-5,12-14H2,1-2H3,(H,24,25)
• chave InChI: HBBVCKCCQCQCTJ-UHFFFAOYSA-N

Descrição

Descrição geral

A cell-permeable phenoxyacetic acid derivative that acts as a potent and selective peroxisome proliferator activator receptor δ (PPARδ) agonist (K_i = 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 (K_i = 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.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
Peroxisome proliferator activator receptor δ (PPAR@delta;)

Product does not compete with ATP.

Reversible: no

Target K_i: 6 nM for hPPARδ and 730 nM for hPPARγ

Embalagem

Packaged under inert gas

Advertência

Toxicity: Irritant (B)

Reconstituição

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Outras notas

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.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable