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 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.|
|Incubation time||12 h|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO ≥ 25 mg/mL|
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