Home Metabolism PCSK9 inhibitor R-IMPP

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R-IMPP PCSK9 inhibitor

Cat.No.S8420

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

Chemical Structure

Molecular Weight: 389.49

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Quality Control

Batch: S842001 DMSO]77 mg/mL]false]Ethanol]77 mg/mL]false]Water]7 mg/mL]false Purity: 99.42%
99.42

Solubility

In vitro
Batch:

DMSO : 77 mg/mL (197.69 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 77 mg/mL

Water : 7 mg/mL

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 389.49 Formula

C24H27N3O2

 Storage (From the date of receipt)
CAS No. 2133832-83-2 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles COC1=CC=C(C=C1)CCC(=O)N(C2CCCNC2)C3=NC=CC4=CC=CC=C43

Mechanism of Action

Targets/IC50/Ki
PCSK9
In vitro
R-IMPP promotes uptake of LDL-C in hepatoma cells by increasing LDL-R levels, without altering levels of secreted transferrin. This compound does not decrease PCSK9 transcription or increase PCSK9 degradation, but instead causes transcript-dependent inhibition of PCSK9 translation. It 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 this chemical is stereospecific.
References

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