product name ZLN005
Description: ZLN005 is a novel, potent and tissue-specific PGC-1α transcriptional activator. In the PGC-1α promoter reporter assay, ZLN005 potently inhibited luciferases. In L6 myotubes, ZLN005 dose-dependently increased PGC-1α mRNA levels. ZLN005 (10 μM) increased the mRNA levels of cytochrome c oxidase 5b (cox5b), acyl-CoA oxidase, strogen-related receptor α (ERRα), NRF1 and GLUT4. ZLN005 (20 μM) increased glucose uptake and oxidation of palmitic acid by 1.8-fold and 1.28-fold respectively in a dose dependent way.
References: Diabetes. 2013 Apr;62(4):1297-307.
250.34
Formula
C17H18N2
CAS No.
49671-76-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 37 mg/mL (147.8 mM)
Water: <1 mg/mL
Ethanol: 2 mg/mL (8 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: In L6 myotubes, ZLN005 increases expression of the PGC-1α gene and downstream genes by activation of AMP-activated protein kinase, and improves glucose uptake and fatty acid oxidation without obvious cytotoxicity. While ZLN005 does not has the same effects in rat primary hepatocytes, which suggests cell type–specificity. Kinase Assay: Cell Assay: In L6 myotubes, ZLN005 dose-dependently increased PGC-1α mRNA levels. ZLN005 (10 μM) increased the mRNA levels of cytochrome c oxidase 5b (cox5b), acyl-CoA oxidase, strogen-related receptor α (ERRα), NRF1 and GLUT4. ZLN005 (20 μM) increased glucose uptake and oxidation of palmitic acid by 1.8-fold and 1.28-fold respectively in a dose dependent way. In L6 myotubes transfected with PGC-1α siRNA, ZLN005-stimulated oxidation of palmitic acid and expression of the PGC-1α gene was blocked. In L6 myotubes, ZLN005 increased the phosphorylation of AMPK and acetyl-CoA carboxylase (ACC). |
|---|---|
| In Vivo | ZLN005 (15 mg/kg, p.o.) produces antihyperglycemia and antihyperlipidemia effects and increases insulin sensitivity in db/db mice but not lean mice. |
| Animal model | Male C57BKS db/db and lean littermate C57BKS mice. |
| Formulation & Dosage | Formulated in 0.5% methylcellulose; 15 mg/kg; p.o. |
| References | Diabetes. 2013 Apr;62(4):1297-307. |
