SR-18292

SKU: orb1223191

Description

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.

Key Properties

• CAS Number: 2095432-55-4
• MW: 366.51
• Purity: >98% (HPLC)
• Formula: C₂₃H₃₀N₂O₂
• SMILES: CC(C)(C)N(Cc1ccc(C)cc1)CC(O)COc3cccc2nccc23
• Target: HDAC
• Solubility: DMSO : ≥ 100 mg/mL; 272.85 mM

Bioactivity

• In Vivo:
  SR-18292 reduces fasting blood glucose, increases hepatic insulin sensitivity and improves glucose homeostasis in diabetic mice. The high fat diet (HFD) fed mice, a dietary model of obesity and T2D, are treated with SR-18292 (45 mg/kg) via i.p. injection for 3 consecutive days and again on day 4 before measuring fasting blood glucose. Strikingly, mice that are treated with SR-18292 have significantly lower levels of fasting blood glucose concentrations compared to matched vehicle-treated control mice. The induction of gluconeogenic gene expression is a regulatory component of the response to fasting. Importantly, gluconeogenic gene expression, specifically that of Pck1, is inhibited in livers isolated from mice treated with SR-18292.
• In Vitro:
  The transcriptional coactivator PGC-1α plays a pivotal role in energy homeostasis by co-activating transcription factors that regulate fat and glucose metabolism. SR-18292 increases the interaction of PGC-1α with the acetyl transferase GCN5 and reduces co-activation of nuclear hormone receptor HNF4α by PGC-1α. SR-18292 suppresses HNF4α/PGC-1α gluconeogenic transcriptional function. By increasing the interaction of GCN5 with PGC-1α, SR-18292 increases the acetylation of specific PGC-1α lysine residues that might subsequently decrease its gluconeogenic activity.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SR-18292 | SR 18292 | SR18292

Quick Database Links

Gene Symbol

HDAC