product name SRT2183
Description: SRT2183 is a small-molecule activator of the sirtuin subtype SIRT1, it is currently being developed by Sirtris Pharmaceuticals as therapeutics for the treatment of type 2 diabetes and potentially leukemia as well. SRT2183 has similar activity in the body to another SIRT1 activator SRT1720 , but is closer in potency to resveratrol. In animal studies it was found to improve insulin sensitivity and lower plasma glucose levels in fat, muscle and liver tissue, and increased mitochondrial and metabolic function. However, the claim that SRT2183 is a SIRT1 activator has been questioned and further defended.
References: Nature. 2007 Nov 29;450(7170):712-6; J Biol Chem. 2010 Mar 12;285(11):8340-51.
468.57
Formula
C27H24N4O2S
CAS No.
1001908-89-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 93 mg/mL (198.5 mM)
Water: <1 mg/mL
Ethanol: 3 mg/mL (6.4 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: SRT2183 is potent with growth arrest and apoptosis induced at doses ranging from 1-20 μM. SRT2183 treatment leads to increased mRNA levels of pro-apoptosis, growth arrest, and DNA damage response genes. SRT1720, SRT2183, SRT1460, and resveratrol exhibit multiple off-target activities against receptors, enzymes, transporters, and ion channels. They are not direct activators of SIRT1. SRT2183 has little or no effect on SIRT1 deacetylating activity with native full-length substrates. SRT2183 activates AMPK, increases Sirt1 expression and decreases RelA/p65 lysine310 acetylation, critical for NF-κB activation, and an established Sirt1 target and inhibits RANKL-induced osteoclast generation and resorptive capacity in bone marrow macrophages. Kinase Assay: Cell Assay: BMMs are harvested, plated and 24-hrs later non-adherent cells were re-plated at a density of 20,000 cells/well in α-MEM/15%FBS/5% M-CSF. For determining cell proliferation, cells are treated with SRT2183 or a vehicle for 72 hours post plating and BrdU reagent is added 48 hrs post SRT2183 or vehicle administration according to the manufacturers instructions to determine cell proliferation 3 days post plating. |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Nature. 2007 Nov 29;450(7170):712-6; J Biol Chem. 2010 Mar 12;285(11):8340-51. |
