Name | R-IMPP |
Synonyms | R-IMPP PF-00932239 (R-IMPP) Benzenepropanamide, N-1-isoquinolinyl-4-methoxy-N-(3R)-3-piperidinyl- |
CAS | 2133832-83-2 |
Molecular Formula | C24H27N3O2 |
Molar Mass | 389.49 |
Density | 1.186±0.06 g/cm3(Predicted) |
Boling Point | 594.4±50.0 °C(Predicted) |
Solubility | DMSO : 41 mg/mL (105.27 mM) |
pKa | 9.14±0.10(Predicted) |
Storage Condition | -20°C |
In vitro study | R-IMPP promotes the uptake of LDL-R in liver cancer cells by increasing the level of LDL-C, without affecting the level of transferrin secretion. R-IMPP does not reduce PCSK9 transcription or increase PCSK9 degradation, but rather results in a transcript-dependent inhibition of PCSK9 translation. R-IMPP had weak anti-PCSK9 secretion activity, IC50 = 4.8 μm. In the recombinant CHO-K1 cells, it did not affect the intracellular ATP level, nor reduce the control protein, secretion of secreted alkaline phosphatase. R-IMPP inhibitory activity with stereo specificity. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.567 ml | 12.837 ml | 25.675 ml |
5 mM | 0.513 ml | 2.567 ml | 5.135 ml |
10 mM | 0.257 ml | 1.284 ml | 2.567 ml |
5 mM | 0.051 ml | 0.257 ml | 0.513 ml |
biological activity | R-IMPP is an inhibitor of PCSK9 secretion, IC50 is 4.8 μM. |
target | TargetValue PCSK9 () |
Target | Value |
In vitro study | R-IMPP promote the absorption of LDL-C in liver cancer cells by increasing the level of LDL-R without affecting the level of transferrin secretion. R-IMPP does not reduce PCSK9 transcription or increase PCSK9 degradation, but causes transcript-dependent inhibition of PCSK9 translation. R-IMPP has weak anti-PCSK9 secretion activity, IC50 = 4.8 μM, and does not affect intracellular ATP level in recombinant CHO-K1 cells, nor does it reduce the secretion of control protein and secretory alkaline phosphatase. The inhibitory activity of R-IMPP is stereospecific. |