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R-IMPP

Cat. No. M6251
R-IMPP Structure
Size Price Availability Quantity
5mg USD 270 In stock
10mg USD 480 In stock
25mg USD 1025 In stock
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Quality Control
  • Current batch:
  • Purity > 99%
  • COA
  • MSDS
Biological Activity

R-IMPP stimulates uptake of LDL-C in hepatoma cells by increasing LDL-R levels, without altering levels of secreted transferrin. R-IMPP does not decrease PCSK9 transcription or increase PCSK9 degradation, but causes transcript-dependent inhibition of PCSK9 translation. R-IMPP is able to selectively bind to human, but not E. coli, ribosomes

Protocol
Cell Experiment
Cell lines Huh7 cells
Preparation method Huh7 cells are plated at 150,000 cells per well and transfected with the full-length and truncation mutants. After 24 hr, cells are treated with vehicle, 30 μMR-IMPP, or 30 μM S-IMPP. At 48 hr post-transfection, cells are washed three times with TBS +2 mg/mL BSA and lysed with 100 mL of RIPA buffer per well. Protein lysates are subjected to SDS-PAGE and western blot analysis for PCSK9 (V5) and b-actin.
Concentrations 10, 30 μM
Incubation time 24 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 389.49
Formula C24H27N3O2
CAS Number
Purity > 99%
Solubility 41 mg/mL in DMSO
Storage at -20°C
References

A Small-Molecule Anti-secretagogue of PCSK9 Targets the 80S Ribosome to Inhibit PCSK9 Protein Translation.
Petersen DN, et al. Cell Chem Biol. 2016 Nov 17;23(11):1362-1371. PMID: 27746128.

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  Catalog
Abmole Inhibitor Catalog 2017




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