Molecular Formula | C19H28ClNO6 |
Molar Mass | 401.88 |
Density | 1.26±0.1 g/cm3(Predicted) |
Melting Point | 90-93°C |
Specific Rotation(α) | D24 -46.6° (c = 0.44 in CHCl3) |
Solubility | DMSO: >15mg/mL |
Appearance | White to light yellow solid |
Color | White to Pale Yellow Waxy |
pKa | 7.19±0.46(Predicted) |
Storage Condition | -20°C |
Stability | Hygroscopic |
In vitro study | No significant difference of apoptotic cell numbers is observed between cells treated with TNP-470 and the controls. The IC 50 s of TNP-470 are 16.86±0.9 µg/mL, 3.16±0.6 µg/mL and 1.78±0.8 µg/mL for KKU-M213 cells at 24, 48 and 72 h, respectively. The results show that TNP-470 significantly reduces the number of migrated cells and invaded cells as compare with the vehicle treated group. TNP-470 decreases the migrated cells of KKU-M213 to 26% and of KKU-M214 to 11% (P<0.01). Similarly, TNP-470 also significantly affects cell invasion, the number of invaded cells is reduced to 25% in KKU-M213 (P<0.01) and to 15% in KKU-M214 (P<0.01). The relative expressions of MMP2 , MMP9 and c-MYC in TNP-470 treated cells are significantly suppressed compare to the vehicle treated cells. |
In vivo study | Treatment with TNP-470 attenuates (P<0.05) liver lipid accumulation compare to high fat fed (HFF) mice. By day 5, TNP-470 treated mice consume significantly less grams of high fat food than vehicle treated HFF mice. By day 15 of treatment, TNP-470 mice are consuming an equivalent number of calories to that of chow fed mice, despite the provision of high fat diet. Treatment with TNP-470 increases (P<0.05) expression of adipose tissue LPL mRNA, compare to chow-fed and high-fat fed controls. TNP-470 decreases energy intake and increases energy expenditure. |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
WGK Germany | 2 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.488 ml | 12.441 ml | 24.883 ml |
5 mM | 0.498 ml | 2.488 ml | 4.977 ml |
10 mM | 0.249 ml | 1.244 ml | 2.488 ml |
5 mM | 0.05 ml | 0.249 ml | 0.498 ml |
Biological activity | TNP-470 is a methionine aminopeptidase -2 inhibitor and an angiogenesis inhibitor. |
target | methionine aminopeptidase-2, angiogenesis |
in vitro study | No significant difference of apoptotic cell numbers is observed between cells treated with TNP-470 and the controls. The IC 50 s of TNP-470 are 16.86±0.9 µg/mL, 3.16±0.6 µg/mL and 1.78±0.8 µg/mL for KKU-M213 cells at 24, 48 and 72 h, respectively. The results show that TNP-470 significantly reduces the number of migrated cells and invaded cells as compare with the vehicle treated group. TNP-470 decreases the migrated cells of KKU-M213 to 26% and of KKU-M214 to 11% (P<0.01). Similarly, TNP-470 also significantly affects cell invasion, the number of invaded cells is reduced to 25% in KKU-M213 (P<0.01) and to 15% in KKU-M214 (P<0.01). The relative expressions of MMP2 , MMP9 and c-MYC in TNP-470 treated cells are significantly suppressed compare to the vehicle treated cells. |
in vivo study | Treatment with TNP-470 attenuates (P<0.05) liver lipid accumulation compare to high fat fed (HFF) mICE. By day 5, TNP-470 treated mICE consume significantly less grams of high fat food than vehicle treated HFF mICE. By day 15 of treatment, TNP-470 mice are consuming an equivalent number of calories to that of chow fed mice, despite the provision of high fat diet. Treatment with TNP-470 increases (P<0.05) expression of adipose tissue LPL mRNA, compare to chow-fed and high-fat fed controls. TNP-470 decreases energy intake and increases energy expenditure. |