Name | SR-18292 |
Synonyms | SR-18292 2-Propanol, 1-[(1,1-dimethylethyl)[(4-methylphenyl)methyl]amino]-3-(1H-indol-4-yloxy)- |
CAS | 2095432-55-4 |
Molecular Formula | C23H30N2O2 |
Molar Mass | 366.5 |
Density | 1.132±0.06 g/cm3(Predicted) |
Boling Point | 553.6±50.0 °C(Predicted) |
Solubility | DMSO : 100 mg/mL (272.85 mM);H2O : < 0.1 mg/mL (insoluble) |
pKa | 13.90±0.20(Predicted) |
Storage Condition | under inert gas (nitrogen or Argon) at 2-8°C |
Physical and Chemical Properties | The bioactive SR-18292 was effective in inhibiting PGC-1α gluconeogenic activity and reducing the co-activation of HNF4α by modulating the interaction of GCN5 and PGC-1α. |
Use | SR-18292 is a PGC-1α inhibitor. SR-18292 reduces blood glucose, strongly increases hepatic insulin sensitivity, and improves glucose homeostasis in dietary and genetic mouse models of T2D. |
Reference Show more | 1: Sharabi K, Lin H, Tavares CD, Dominy JE, Camporez JP, Perry RJ, Schilling R,Rines AK, Lee J, Hickey M, Bennion M, Palmer M, Nag PP, Bittker JA, Perez J,Jedrychowski MP, Ozcan U, Gygi SP, Kamenecka TM, Shulman GI, Schreiber SL,Griffin PR, Puigserver P. Selective Chemical Inhibition of PGC-1α Gluconeogenic Activity Ameliorates Type 2 Diabetes. Cell. 2017 Mar 23;169(1):148-160.e15. doi:10.1016/j.cell.2017.03.001. PubMed PMID: 28340340. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.729 ml | 13.643 ml | 27.285 ml |
5 mM | 0.546 ml | 2.729 ml | 5.457 ml |
10 mM | 0.273 ml | 1.364 ml | 2.729 ml |
5 mM | 0.055 ml | 0.273 ml | 0.546 ml |
Target
Target Value
PGC-1α
in vitro studies
In hepatocytes, SR-18292 is an effective inhibitor of gluconeogenesis-related gene expression and glucose production. It can increase the interaction between PGC-1α and GCN5 and reduce the synergistic activation of HNF4α through PGC-1α. SR-18292 inhibits the transcriptional function of HNF4α/PGC-1α gluconeogenesis.
In vivo studies
in dietary and hereditary mouse models with type 2 diabetes, SR-18292 can reduce blood sugar, strongly increase liver insulin sensitivity and improve glucose homeostasis. In the body, SR-18292 can inhibit the production of glucose in the liver. The main target organ of SR-18292 in the body is the liver, which is an important part of its anti-diabetic activity.