Molecular Formula | C22H26O7 |
Molar Mass | 402.44 |
Density | 1.222±0.06 g/cm3(Predicted) |
Melting Point | 127-128°C(lit.) |
Boling Point | 600.8±55.0 °C(Predicted) |
Solubility | DMSO: >10mg/mL |
Appearance | solid |
Color | off-white |
pKa | 3.23±0.10(Predicted) |
Storage Condition | 2-8°C |
Stability | Light Sensitive |
MDL | MFCD04974501 |
In vitro study | L-165041 is a PPARδ agonist, with K i s of 6 nM and appr 730 nM for PPARδ and PPARγ, respectively. L-165041 (1 or 5 µM) inhibits VEGF-induced endothelial cells (ECs) proliferation and migration. L-165041 negatively affects cell cycle progression in VEGF-activated human umbilical vein ECs (HUVECs). L-165041 (10 µM)inhibits PPARδ-independent, VEGF-induced angiogenesis. PPARδ ligand L-165041 inhibits PDGF-induced rVSMC proliferation and migration. With 1 h of L-165041 pretreatment, PDGF-induced cellular migration is inhibited. L-165041 (10 μM) significantly suppresses S phase transition induced by PDGF. |
In vivo study | L-165041 (5 mg/kg/day, i.p.) significantly lowers the formation of lipid droplets in mice. L-165041 markedly reduces the level of both the hepatic cholesterol and triglycerides in mice. L-165041 increases mRNA expression levels of PPARδ compared to the vehicle group. Lipoprotein lipase (LPL) expression in L-165041-treated mice is significantly higher than that in the vehicle group. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.485 ml | 12.424 ml | 24.848 ml |
5 mM | 0.497 ml | 2.485 ml | 4.97 ml |
10 mM | 0.248 ml | 1.242 ml | 2.485 ml |
5 mM | 0.05 ml | 0.248 ml | 0.497 ml |
biological activity | L-165041 is a cell-penetrating pparδ agonist, ki values for pparδ and PPARγ are 6 nM and about 730 nM, respectively, and can induce adipocyte differentiation in NIH-pparδ cells. |
Target | PPAR δ 6 nM (Ki) PPAR γ 730 nM (Ki) |
in vitro study | L-165041 is is a PPAR δ agonist, with K I s of 6 nM and appr 730 nM for PPAR δ and PPAR γ, review. L-165041 (1 or 5 µm) traits VEGF-induced endothlial cells (ECs) propagation and migration. L-165041 cellular effects cell cycle progression in VEGF-activated human umbilical vein ECs (HUVECs). L-165041 (10 μm), VEGF-induced angiogenesis. PPARδ ligand L-165041 inhibits PDGF-induced rVSMC proliferation and migration. With 1 h of L-165041 pretreatment, PDGF-induced cellular migration is inhibited. L-165041 (10 μM) significantly suppresses S phase transition induced by PDGF. |
in vivo study | L-165041 (5 mg/kg/day, I. p.) the formation of lipid droplets in mice. L-165041 marked mice. L-165041 increases mRNA expression levels of PPARδ compared to the vehicle group. Lipoprotein lipase (LPL) expression in L-165041-treated mice is significantly higher than that in the vehicle group. |