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R-IMPP

Name: R-IMPP
Brand: TargetMol
SKU: T4058
Price: 40 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T4058Cas No. 2133832-83-2

R-IMPP is an inhibitor of PCSK9 translation. R-IMPP stimulates uptake of LDL-C in hepatoma cells by increasing LDL-R levels, without altering levels of secreted transferrin.

R-IMPP

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Purity: 99.85%

Catalog No. T4058Cas No. 2133832-83-2

R-IMPP is an inhibitor of PCSK9 translation. R-IMPP stimulates uptake of LDL-C in hepatoma cells by increasing LDL-R levels, without altering levels of secreted transferrin.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$40	In Stock	In Stock
2 mg	$54	In Stock	In Stock
5 mg	$85	In Stock	In Stock
10 mg	$150	In Stock	In Stock
25 mg	$312	In Stock	In Stock
50 mg	$555	In Stock	In Stock
100 mg	$798	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$73	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.85%

Color:Yellow

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COA HNMR LCMS

Product Introduction

R-IMPP AI Summary

R-IMPP demonstrates multiple bioactivities, including moderate lipophilicity with a LogD of 1.1 and moderate apparent permeability in RRCK cells (Papp = 5.4 x 10^-6 cm/s). It shows high intrinsic clearance in rat liver microsomes (CL > 510.0 mL.min^-1.g^-1) and moderate clearance in human liver microsomes (CL = 20.6 mL.min^-1.g^-1). This compound exhibits negligible inhibition of several CYP enzymes (CYP1A2, CYP2D6, CYP2C9, CYP3A4) at a concentration of 3 µM and weak inhibition of dofetilide binding to human ERG with a Ki of 13000.0 nM. Furthermore, it demonstrates moderate binding affinity to the 80S ribosome in HuH7 cells, inhibiting PCSK9 mRNA translation with IC50 values of 2630.0 nM (luciferase reporter assay) and 8370.0 nM (ELISA). Its activity in inhibiting human PCSK9 expression is also confirmed by an IC50 value of 2200.0 nM in an ELISA assay. In CHOK1 cells, R-IMPP reduces PL-tagged PCSK9 expression with an IC50 of 4800.0 nM. Additionally, the compound is not significantly cytotoxic, with an IC50 greater than 20000.0 nM against rat bone marrow cells..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	R-IMPP is an inhibitor of PCSK9 translation. R-IMPP stimulates uptake of LDL-C in hepatoma cells by increasing LDL-R levels, without altering levels of secreted transferrin.
Targets&IC50	PCSK9:4.8 μM (IC50)

Chemical Properties

Molecular Weight	389.49
Formula	C₂₄H₂₇N₃O₂
Cas No.	2133832-83-2
Smiles	COc1ccc(CCC(=O)N([C@@H]2CCCNC2)c2nccc3ccccc23)cc1
Relative Density.	1.186 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature | Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 70 mg/mL (179.72 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.13 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.5675 mL	12.8373 mL	25.6746 mL	128.3730 mL
5 mM	0.5135 mL	2.5675 mL	5.1349 mL	25.6746 mL
10 mM	0.2567 mL	1.2837 mL	2.5675 mL	12.8373 mL
20 mM	0.1284 mL	0.6419 mL	1.2837 mL	6.4187 mL
50 mM	0.0513 mL	0.2567 mL	0.5135 mL	2.5675 mL
100 mM	0.0257 mL	0.1284 mL	0.2567 mL	1.2837 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc