L-165041
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
对PPARγ的Ki值为6 nM。
过氧化物酶体增殖物激活受体(PPARγ)广泛表达,参与脂质和葡萄糖代谢。研究表明,PPARγ表达于内皮细胞,在内皮细胞增殖与存活中起着重要作用。据报道,L-165041是选择性的和有效的PPARγ配体。
体外:除了具有高度有效的PPARδ激动剂活性、PPARγ2部分激动作用以及PPARα完全激动作用,L-165041还是选择性的和有效的PPARγ配体,参与特定的转录激活系统[1]。
体内:相对于安慰剂组,L-165041可以显著抑制脂质在小鼠肝脏中堆积,并降低肝脏总甘油三酯以及胆固醇含量。基因分析表明,L-165041降低肝脏PPARγ、载脂蛋白B、白介素1β和白介素6的表达。与此相反,L-165041增加肝脏PPARδ、脂蛋白脂肪酶以及ATP结合盒转运蛋白G1(ABCG1)的表达[2]。
临床试验:到目前为止,L-165041还处于临床前开发阶段。
参考文献:
[1] Wurch T, Junquero D, Delhon A, Pauwels J. Pharmacological analysis of wild-type alpha, gamma and delta subtypes of the human peroxisome proliferator-activated receptor. Naunyn Schmiedebergs Arch Pharmacol. 2002 Feb;365(2):133-40.
[2] Lim HJ, Park JH, Lee S, Choi HE, Lee KS, Park HY. PPARdelta ligand L-165041 ameliorates Western diet-induced hepatic lipid accumulation and inflammation in LDLR-/- mice. Eur J Pharmacol. 2009 Nov 10;622(1-3):45-51.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 402.44 |
Cas No. | 79558-09-1 |
Formula | C22H26O7 |
Synonyms | L 165041;L165041 |
Solubility | ≥40.2 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
Chemical Name | 2-[4-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propoxy]phenoxy]acetic acid |
SDF | Download SDF |
Canonical SMILES | CCCC1=C(C=CC(=C1O)C(=O)C)OCCCOC2=CC=C(C=C2)OCC(=O)O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Description | L-165041是有效的PPARδ激动剂,其Ki值为6 nM。 | |||||
靶点 | PPARδ | |||||
IC50 | 6 nM (Ki) |
质量控制和MSDS
- 批次: