L-165041

中文名称:

L-165041

中文同义词:

[4-[3-(4-乙酰基-3-羟基-2-丙基苯氧基)丙氧基]苯氧基]乙酸

英文名称:

L-165,041

英文同义词:

4-[3-(2-PROPYL-3-HYDROXY-4-ACETYL)PHENOXY]PROPYLOXYPHENOXY-ACETIC ACID;4-[3-(4-ACETYL-3-HYDROXY-2-PROPYLPHENOXY)PROPOXY]PHENOXYACETIC ACID;L-165,041;COMPOUND P;L 1q5041;Acetic acid, 2-[4-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propoxy]phenoxy]-;2-(4-(3-(4-acetyl-3-hydroxy-2-propylphenoxy)propoxy)phenoxy)acetic acid;2-[4-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propoxy]phenoxy]-

CAS号:

79558-09-1

分子式:

C22H26O7

分子量:

402.44

EINECS号:

相关类别:

医药中间体;细胞生物学;Intracellular receptor;API

Mol文件:

79558-09-1.mol

熔点 

127-128 °C(lit.)

沸点 

600.8±55.0 °C(Predicted)

密度 

1.222±0.06 g/cm3(Predicted)

储存条件 

2-8°C

溶解度 

DMSO: >10 mg/mL

酸度系数(pKa)

3.23±0.10(Predicted)

形态

solid

颜色

off-white

生物活性

L-165041 是一种细胞渗透的 PPARδ 激动剂，对 PPARδ 和 PPARγ 的 Ki 值分别为 6 nM 和 约 730 nM，可以在 NIH-PPARδ 细胞中诱导脂肪细胞分化。

靶点

PPARδ 6 nM (Ki) PPARγ 730 nM (Ki)

PPARδ 6 nM (Ki)

PPARγ 730 nM (Ki)

体外研究

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.

体内研究

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 

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