79558-09-1 Usage
Description
L-165,041 is a cell-permeable phenoxyacetic acid derivative that acts as a potent and selective peroxisome proliferator-activated receptor δ (PPARδ) agonist. It has a Ki value of 6 nM for human PPARδ and 730 nM for human PPARγ. L-165,041 has been used to study its influence on PPARβ/δ mediated postnatal myogenesis in C2C12 myoblasts.
Uses
Used in Pharmaceutical Research:
L-165,041 is used as a PPARβ/δ ligand for studying its influence on PPARβ/δ mediated postnatal myogenesis in C2C12 myoblasts. This helps researchers understand the role of PPARβ/δ in muscle development and regeneration.
Used in Cell Biology:
L-165,041 is used to potently induce adipocyte differentiation in NIH-PPARδ cells at a concentration of 500 nM. This application aids in studying the process of adipogenesis and the role of PPARδ in this cellular differentiation.
Used in Metabolic Research:
L-165,041 is used to raise total cholesterol levels in insulin-resistant db/db mice without altering glucose or triglyceride levels. This application helps researchers investigate the effects of PPARδ activation on lipid metabolism and its potential implications in the treatment of dyslipidemia.
Used in Molecular Biology:
L-165,041 is used to increase the expression of the UCP3 (uncoupling protein 3) gene in L6 myotubes. This application is valuable for studying the role of PPARδ in the regulation of genes involved in energy metabolism and thermogenesis.
Used in Inflammation Research:
L-165,041 is used to inhibit cytokine-induced expression of VCAM-1 (vascular cell adhesion molecule-1) and the secretion of MCP-1 (monocyte chemotactic protein-1) in EAhy926 cells. This application is useful for investigating the anti-inflammatory effects of PPARδ activation and its potential role in modulating immune responses.
Biological Activity
Potent PPAR δ agonist (K i = 6 nM); displays > 100-fold selectivity for both mouse and human PPAR δ ? receptors over other subtypes. In vivo, raises plasma cholesterol levels in insulin-resistant db/db mice and is neuroprotective in models of cerebral infarction and Parkinson's disease.
Biochem/physiol Actions
Cell permeable: yes
in vitro
l-165041, which is a selective and potent pparδligand, displayed in this specified transactivation system, apart from its highly efficacious pparδ agonist activity, partial and full agonism at, respectively, pparγ2 and pparαsubtypes [1].
in vivo
l-165041 could drastically reduce lipid accumulation in the mouse liver, decreasing total hepatic triglyceride and cholesterol content compared to the vehicle group. gene analysis demonstrated that l-165041 lowered hepatic expression of pparγ, apolipoprotein b, il-1β, and interleukin-6. in contrast, l-165041 increased hepatic expressions of pparδ, lipoprotein lipase, and atp-binding cassette transporter g1 (abcg1) [2].
references
[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.
Check Digit Verification of cas no
The CAS Registry Mumber 79558-09-1 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 7,9,5,5 and 8 respectively; the second part has 2 digits, 0 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 79558-09:
(7*7)+(6*9)+(5*5)+(4*5)+(3*8)+(2*0)+(1*9)=181
181 % 10 = 1
So 79558-09-1 is a valid CAS Registry Number.
InChI:InChI=1/C22H26O7/c1-2-4-19-20(10-5-16(11-12-23)22(19)26)28-14-3-13-27-17-6-8-18(9-7-17)29-15-21(24)25/h5-10,12,26H,2-4,11,13-15H2,1H3,(H,24,25)