SRT2104

SKU: orb1222878

Description

SRT2104, also known as GSK2245840, is a novel, first-in-class, highly selective small molecule activator of the NAD + dependent deacetylase SIRT1. SRT2104 has been developed as a selective small molecule activator of SIRT1, a NAD(+)-dependent deacetylase involved in the regulation of energy homeostasis and the modulation of various metabolic pathways, including glucose metabolism, oxidative stress and lipid metabolism. SIRT1 has been suggested as putative therapeutic target in multiple age-related diseases including type 2 diabetes and dyslipidemias.(In Vivo):SRT 2104 (100 mg/kg/day, supplemented in diet for 24 weeks) increases SIRT1 protein without altering Sirt1 mRNA in diabetic mice.SRT 2104 (100 mg/kg/day, supplemented in diet for 24 weeks) decreases testicular oxidative stress, activation of apoptotic signaling, and ER stress in diabetic mice.SRT 2104 (0.5%; for 18 weeks) improves motor function and increases survival in N171-82Q HD mice.

Key Properties

• CAS Number: 1093403-33-8
• MW: 516.64
• Purity: >98% (HPLC)
• Formula: C₂₆H₂₄N₆O₂S₂
• SMILES: Cc1c(sc(n1)c1cnccc1)C(=O)Nc1ccccc1c1cn2c(csc2n1)CN1CCOCC1
• Target: DNA/RNA Synthesis
• Solubility: DMSO : 5 mg/mL 9.68 mM; H2O : < 0.1 mg/mL

Bioactivity

• In Vivo:
  SRT 2104 (100 mg/kg/day, supplemented in diet for 24 weeks) increases SIRT1 protein without altering Sirt1 mRNA in diabetic mice. SRT 2104 (100 mg/kg/day, supplemented in diet for 24 weeks) decreases testicular oxidative stress, activation of apoptotic signaling, and ER stress in diabetic mice. SRT 2104 (0.5%; for 18 weeks) improves motor function and increases survival in N171-82Q HD mice. Animal model: Male C57BL/6 mice (8-week-old). Dosage: 100 mg/kg/day. Administration: Supplemented in diet for 24 weeks. Result: Enhanced SIRT1 protein without evelating Sirt1 mRNA level. Attenuated diabetes mellitus (DM)-induced oxidative stress, apoptotic signaling, and ER stress. Animal model: WT and N171-82Q HD mice (6 weeks old). Dosage: 0.5%. Administration: 0.5% SRT 2104 containing diet for 6, 12, 18 weeks. Result: Ameliorated motor deficits and increased survival in N171-82Q HD mice.

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

SRT2104 | SRT 2104 | SRT-2104 | GSK2245840

Quick Database Links

Gene Symbol

DNA/RNA Synthesis