SRT2104 (GSK2245840)

Catalog No.S7792

For research use only.

SRT2104 (GSK2245840) is a selective SIRT1 activator involved in the regulation of energy homeostasis. Phase 2.

SRT2104 (GSK2245840) Chemical Structure

CAS No. 1093403-33-8

Selleck's SRT2104 (GSK2245840) has been cited by 11 Publications

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Biological Activity

Description SRT2104 (GSK2245840) is a selective SIRT1 activator involved in the regulation of energy homeostasis. Phase 2.
Targets
SIRT1 [1]
In vitro

SRT2104 reduces p65/RelA acetylation levels in C2C12 cells.[1]

In vivo In male C57BL/6J mice, SRT2104 (100 mg/kg, p.o.) extends both mean and maximal lifespan of mice fed a standard diet, and enhances motor coordination, bone mineral density, and insulin sensitivity and decreased inflammation. Short-term SRT2104 treatment preserves bone and muscle mass in an experimental model of atrophy.[1] In Male N171-82Q HD mice, SRT2104 (diet containing 0.5% SRT2104) effectively penetrates the blood-brain barrier, attenuates brain atrophy, improves motor function, and extends survival.[2]

Protocol (from reference)

Kinase Assay:[3]
  • SIRT1 fluorescence polarization assay and HTS:

    In the SIRT1 FP assay, SIRT1 activity is monitored using a 20 amino acid peptide (Ac-Glu-Glu-Lys(biotin)-Gly-Gln-Ser-Thr-Ser-Ser-His-Ser-Lys(Ac)-Nle-Ser-Thr-Glu-Gly–Lys(MR121 or Tamra)-Glu-Glu-NH2 ) derived from the sequence of p53. The peptide is N-terminally linked to biotin and C-terminally modified with a fluorescent tag. The reaction for monitoring enzyme activity is a coupled enzyme assay where the first reaction is the deacetylation reaction catalyzed by SIRT1 and the second reaction is cleavage by trypsin at the newly exposed lysine residue. The reaction is stopped and streptavidin is added in order to accentuate the mass differences between substrate and product. The fluorescence polarization reaction conditions are as follows: 0.5 μM peptide substrate, 150 μM βNAD +, 0-10 nM SIRT1, 25 mM Tris-acetate pH 8, 137 mM Na-Ac, 2.7 mM K-Ac, 1 mM Mg-Ac, 0.05% Tween-20, 0.1% Pluronic F127, 10 mM CaCl 2 , 5 mM DTT, 0.025% BSA, and 0.15 mM nicotinamide. The reaction is incubated at 37°C and stopped by addition of nicotinamide, and trypsin is added to cleave the deacetylated substrate. This reaction is incubated at 37 ℃ in the presence of 1 μM streptavidin. Fluorescent polarization is determined at excitation (650 nm) and emission (680 nm) wavelengths.

Cell Research:[1]
  • Cell lines: C2C12 cell line
  • Concentrations: 3 μM
  • Incubation Time: 24 h
  • Method: Cells are cultured in low glucose Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum and penicillin–streptomycin. Cells are treated with vehicle (0.1% DMSO) or 3 μM SRT2104 for 24 h and then harvested for protein and Western blotting.
Animal Research:[2]
  • Animal Models: Male N171-82Q HD mice
  • Dosages: diet containing 0.5% SRT2104
  • Administration: p.o.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 516.64
Formula

C26H24N6O2S2

CAS No. 1093403-33-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(SC(=N1)C2=CN=CC=C2)C(=O)NC3=CC=CC=C3C4=CN5C(=CSC5=N4)CN6CCOCC6

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01453491 Completed Drug: SRT2104 Colitis Ulcerative Sirtris a GSK Company|GlaxoSmithKline February 13 2012 Phase 1
NCT01039909 Withdrawn Drug: Placebo|Drug: SRT2104 Healthy Volunteer|Atrophy Muscular GlaxoSmithKline January 2011 Phase 1
NCT01154101 Completed Drug: Placebo|Drug: SRT2104 Psoriasis Sirtris a GSK Company|GlaxoSmithKline June 7 2010 Phase 2
NCT01031108 Completed Drug: Placebo|Drug: SRT2104 Diabetes Mellitus Type 2 Sirtris a GSK Company|GlaxoSmithKline May 28 2010 Phase 1
NCT01018017 Completed Drug: Placebo|Drug: SRT2104 Diabetes Mellitus Type 2 GlaxoSmithKline March 3 2010 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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