Molecular Weight(MW): 516.64
SRT2104 (GSK2245840) is a selective SIRT1 activator involved in the regulation of energy homeostasis. Phase 2.
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|Description||SRT2104 (GSK2245840) is a selective SIRT1 activator involved in the regulation of energy homeostasis. Phase 2.|
SRT2104 reduces p65/RelA acetylation levels in C2C12 cells.
|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. 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.|
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.
|In vitro||DMSO||16 mg/mL warmed (30.96 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01702493||Completed||Psoriasis||Sirtris, a GSK Company|GlaxoSmithKline||October 2012||Phase 1|
|NCT01453491||Completed||Colitis, Ulcerative||Sirtris, a GSK Company|GlaxoSmithKline||February 2012||Phase 1|
|NCT01039909||Withdrawn||Healthy Volunteer|Atrophy, Muscular||GlaxoSmithKline||January 2011||Phase 1|
|NCT01154101||Completed||Psoriasis||Sirtris, a GSK Company|GlaxoSmithKline||June 2010||Phase 2|
|NCT01031108||Completed||Diabetes Mellitus, Type 2||Sirtris, a GSK Company|GlaxoSmithKline||May 2010||Phase 1|
|NCT01018017||Completed||Diabetes Mellitus, Type 2||GlaxoSmithKline||March 2010||Phase 2|
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