3-TYP is a selective SIRT3 inhibitor with an IC50 value of 16 nM, which is more potent over SIRT1 and SIRT2. 3-TYP significantly attenuates melatonin-induced increases in deacetylated-SOD2 expression and SOD2 activity in HepG2 cells exposed to Cd.
In vivo, 3-TYP significantly decreases SIRT3 activity and increases the acetylation of SOD2 compared with that in the control group, without influencing SIRT3 expression. 3-TYP attenuates the cardioprotective effects of melatonin by decreasing the LVEF and LVFS after 24 hour of reperfusion. 3-TYP also increases the infarct size, serum LDH levels, and apoptotic ratio compared with those in the IR+Mel group.
| Cell Experiment | |
|---|---|
| Cell lines | HepG2 cells |
| Preparation method | Cells are randomly divided into the following treatment groups: 10 μM Cd; melatonin (1 μM)+10 μM Cd; 3-TYP (50 μM)+10 μM Cd; and 3-TYP (50 μM)+melatonin (1 μM)+10 μM Cd. cells are treated for 12 h. The role of the SIRT3-SOD2 pathway in hepatic cell protection after melatonin pretreatment is investigated. |
| Concentrations | 50 μM |
| Incubation time | 12 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 146.15 |
| Formula | C7H6N4 |
| CAS Number | 120241-79-4 |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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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