Molecular Formula | C7H6N4 |
Molar Mass | 146.15 |
Density | 1.296±0.06 g/cm3(Predicted) |
Melting Point | 180-182 °C(Solv: ethyl acetate (141-78-6); ethyl ether (60-29-7)) |
Boling Point | 386.6±17.0 °C(Predicted) |
pKa | 7.54±0.70(Predicted) |
Storage Condition | 2-8°C |
In vitro study | In HepG2 cells exposed to cadmium, 3-TYP attenuated the melatonin-induced increase in deacetylated SOD2 expression and inhibited SOD2 activity. |
In vivo study | 3-TYP (50 mg/kg, i.p.) does not significantly influence the LVEF, LVFS, infarct size, serum LDH levels, apoptosis, and oxidative stress compared with those of the Sham group. Moreover, 3-TYP has little effect on gp91phox, Nrf2, NQO 1, Bax, Bcl-2, Caspase-3, and cleaved Caspase-3 expression levels, compared with the Sham group. 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 6.842 ml | 34.212 ml | 68.423 ml |
5 mM | 1.368 ml | 6.842 ml | 13.685 ml |
10 mM | 0.684 ml | 3.421 ml | 6.842 ml |
5 mM | 0.137 ml | 0.684 ml | 1.368 ml |
biological activity | 3-TYP (3-(1H-1,2,3-triazol-4-yl) pyridine) is a selective inhibitor of SIRT3. Compared with Sirt1 and Sirt2, it has higher selectivity for Sirt3. The IC50 for SIRT1, SIRT2 and SIRT3 is 88 nM, 92 nM and 16 nM respectively. |
target | TargetValue SIRT3 (cell-free) 16 nM SIRT1 (cell-free) 88 nM SIRT2 (cell-free) 92 nM |
Target | Value |
SIRT3 (cell-free) | 16 nM |
SIRT1 (cell-free) | 88 nM |
SIRT2 (cell-free) | 92 nM |
in vitro study | In HepG2 cells exposed to cadmium, 3-TYP can attenuate the increased expression of deacetylated SOD2 induced by melatonin and inhibit SOD2 activity. |
in vivo study | 3-TYP (50 mg/kg, I. p.) does not significantly influence the LVEF, LVFS, infarct size, serum LDH levels, apoptosis, and oxidative stress compared with those of the Sham group. Moreover, 3-TYP has little effect on gp91phox, Nrf2, NQO 1, Bax, Bcl-2, Caspase-3, and cleaved Caspase-3 expression levels, compared with the Sham group. 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. |