R-IMPP

For research use only.

Catalog No.S8420

R-IMPP Chemical Structure

Molecular Weight(MW): 389.49

R-IMPP is an inhibitor of PCSK9 secretion, half maximal inhibitory concentration [IC50] = 4.8 μM.

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Choose Selective PCSK9 Inhibitors

Biological Activity

Description R-IMPP is an inhibitor of PCSK9 secretion, half maximal inhibitory concentration [IC50] = 4.8 μM.
Targets
PCSK9 [1]
()
In vitro

R-IMPP promotes 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 instead causes transcript-dependent inhibition of PCSK9 translation. R-IMPP is discovered that exhibited weak PCSK9 anti-secretagogue activity (half maximal inhibitory concentration [IC50] = 4.8 μM), but does not affect intracellular ATP levels in the recombinant CHO-K1 cells, a measure of cytotoxicity, nor decrease secretion of a control protein, secreted alkaline phosphatase, a measure of relative selectivity. The inhibitory response of R-IMPP is stereospecific[1].

Protocol

Cell Research:

[1]

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  • Cell lines: Huh7 cells
  • Concentrations: 10, 30 μM
  • Incubation Time: 24 h
  • 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.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 77 mg/mL (197.69 mM)
Ethanol 77 mg/mL (197.69 mM)
Water 7 mg/mL (17.97 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 389.49
Formula

C24H27N3O2

CAS No. 2133832-83-2
Storage powder
in solvent
Synonyms N/A
Smiles COC1=CC=C(CCC(=O)N(C2CCCNC2)C3=C4C=CC=CC4=CC=N3)C=C1

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID