SRT1720 is a selective small molecule activator of SIRT1 that is 1,000-fold more potent than resveratrol (EC1.5 = 0.16 versus 46.2 µM, respectively). SRT1720 increased the activity of SIRT1 and AMPKα phosphorylation at Ser485 via the cAMP-protein kinase A (PKA) pathway. Treatment of MM cells with SRT1720 inhibited growth and induced apoptosis in MM cells resistant to conventional and bortezomib therapies without significantly affecting the viability of normal cells. Mechanistic studies showed that anti-MM activity of SRT1720 is associated with: (i) activation of caspase-8, caspase-9, caspase-3, poly(ADP) ribose polymerase; (ii) increase in reactive oxygen species; (iii) induction of phosphorylated ataxia telangiectasia mutated/checkpoint kinase 2 signalling; (iv) decrease in vascular endothelial growth factor-induced migration of MM cells and associated angiogenesis; and (v) inhibition of nuclear factor-κB. Blockade of ATM attenuated SRT1720-induced MM cell death. Finally, SRT1720 enhanced the cytotoxic activity of bortezomib or dexamethasone.
Oxid Med Cell Longev. 2022 Jul 18;2022:5961123.
Nicotinamide Mononucleotide Ameliorates Cellular Senescence and Inflammation Caused by Sodium Iodate in RPE
SRT1720 Hydrochloride purchased from AbMole
 |
Source | Cell Rep (2014). Figure 1.SRT1720 |
| Method | gavage | |
| Cell Lines | Male C57BL/6J mice | |
| Concentrations | 1.33g/kg | |
| Incubation Time | ||
| Results | The hazard ratio for death was significantly reduced with SRT1720 treatment (HR=0.73, 95% CI (0.59, 0.90)], p=0.0034), indicating a positive effect of SRT1720 on improving lifespan in mice. SRT1720 significantly reduced the average body weight of HFD-fed mice despite no difference in daily caloric intake or food consumption. |
| Cell Experiment | |
|---|---|
| Cell lines | 4T1 cells |
| Preparation method | Cell viability assay. One day before treatment, 1.5x104 cells per well were seeded in a 96-well plate and allowed to attach overnight. The cells were then treated with varying concentrations of SRT1720 for 24 h. The viable cell number was determined with an MTS assay kit (Promega, Madison, WI, USA). |
| Concentrations | 0~5 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | 4T1 cells tumor-bearing mice model |
| Formulation | water |
| Dosages | 100 mg/kg 5 times per week |
| Administration | orally |
| Molecular Weight | 506.02 |
| Formula | C25H23N7OS.HCl |
| CAS Number | 1001645-58-4 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage | -20°C, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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