R-IMPP (Synonyms: PF-00932239)

Name: R-IMPP
Brand: MedChemExpress
SKU: HY-101354
Rating: 4.5 (1 reviews)

Cat. No.: HY-101354 Purity: 98.42%: FAQs
Data Sheet SDS COA Handling Instructions

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R-IMPP (PF-00932239) is an anti-secretagogue of PCSK9 (IC₅₀=4.8 μM), which targets the 80S ribosome to inhibit PCSK9 protein translation.

For research use only. We do not sell to patients.

R-IMPP Chemical Structure

CAS No. : 2133832-83-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 121	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 121	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 52	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 198	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 418	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 748	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
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Description

R-IMPP (PF-00932239) is an anti-secretagogue of PCSK9 (IC₅₀=4.8 μM), which targets the 80S ribosome to inhibit PCSK9 protein translation^[1].

IC₅₀ & Target

IC50: 4.8 μM (PCSK9)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
Bone marrow cell	IC₅₀	> 20 μM Compound: 1; PF-00932239	Cytotoxicity against rat bone marrow cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Cytotoxicity against rat bone marrow cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 29878763]
CHO-K1	IC₅₀	< 10 μM Compound: 1; R-IMPP, PF-00932239	Inhibition of human recombinant full length ProLabel-tagged PCSK9 expressed in CHO-K1 cells incubated overnight and measured after 3 days by chemiluminescence assay Inhibition of human recombinant full length ProLabel-tagged PCSK9 expressed in CHO-K1 cells incubated overnight and measured after 3 days by chemiluminescence assay	[PMID: 30448414]
CHO-K1	IC₅₀	> 10 μM Compound: 1; R-IMPP, PF-00932239	Inhibition of human recombinant PCSK9 expressed in CHO-K1 cells assessed as alkaline phosphatase secretion incubated overnight and measured after 3 days by HTS assay Inhibition of human recombinant PCSK9 expressed in CHO-K1 cells assessed as alkaline phosphatase secretion incubated overnight and measured after 3 days by HTS assay	[PMID: 30448414]
CHO-K1	IC₅₀	> 10 μM Compound: 1; R-IMPP, PF-00932239	Cytotoxicity against CHOK1 cells expressing human recombinant full length ProLabel-tagged PCSK9 after overnight incubation by CellTiter blue assay Cytotoxicity against CHOK1 cells expressing human recombinant full length ProLabel-tagged PCSK9 after overnight incubation by CellTiter blue assay	[PMID: 30448414]
CHO-K1	IC₅₀	4.8 μM Compound: 1; R-IMPP, PF-00932239	Inhibition of human recombinant full length ProLabel-tagged PCSK9 expressed in CHO-K1 cells incubated overnight and measured after 3 days by HTS assay Inhibition of human recombinant full length ProLabel-tagged PCSK9 expressed in CHO-K1 cells incubated overnight and measured after 3 days by HTS assay	[PMID: 30448414]
CHO-K1	IC₅₀	4.8 μM Compound: Fig 8, Cpd 80S	Inhibition of 80s ribosome in CHOK1 cells assessed as reduction in PL-tagged PCSK9 expression incubated for over night by EFC kit method Inhibition of 80s ribosome in CHOK1 cells assessed as reduction in PL-tagged PCSK9 expression incubated for over night by EFC kit method	[PMID: 31673315]
HeLa	IC₅₀	8.04 μM Compound: 1; PF-00932239	Binding affinity to 80S ribosome in human HeLa cells lysates using human full length PCSK9 encoding mRNAs assessed as inhibition of PCSK9 mRNA translation after 45 mins by Steady-Glo luciferase reporter gene assay Binding affinity to 80S ribosome in human HeLa cells lysates using human full length PCSK9 encoding mRNAs assessed as inhibition of PCSK9 mRNA translation after 45 mins by Steady-Glo luciferase reporter gene assay	[PMID: 30482620]
Huh-7	IC₅₀	2.2 μM Compound: 13; R-IMPP	Inhibition of PCSK9 expression in human HuH7 cells after overnight incubation by ELISA Inhibition of PCSK9 expression in human HuH7 cells after overnight incubation by ELISA	[PMID: 29519739]
Huh-7	IC₅₀	2.63 μM Compound: 1; PF-00932239	Binding affinity to 80S ribosome in human HuH7 cells harboring human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay Binding affinity to 80S ribosome in human HuH7 cells harboring human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay	[PMID: 30482620]
Huh-7	IC₅₀	2.63 μM Compound: 1; PF-00932239	Binding affinity to 80S ribosome in human HuH7 cells harboring pCMV-truncated human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay Binding affinity to 80S ribosome in human HuH7 cells harboring pCMV-truncated human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay	[PMID: 29878763]
Huh-7	IC₅₀	8.37 μM Compound: 1; PF-00932239	Binding affinity to 80S ribosome in human HuH7 cells assessed as inhibition of PCSK9 mRNA translation after overnight incubation by ELISA Binding affinity to 80S ribosome in human HuH7 cells assessed as inhibition of PCSK9 mRNA translation after overnight incubation by ELISA	[PMID: 29878763]

In Vitro

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

389.49

Formula

C₂₄H₂₇N₃O₂

CAS No.

2133832-83-2

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N(C1=NC=CC2=C1C=CC=C2)[C@H]3CNCCC3)CCC4=CC=C(OC)C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (256.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5675 mL	12.8373 mL	25.6746 mL
5 mM	0.5135 mL	2.5675 mL	5.1349 mL
10 mM	0.2567 mL	1.2837 mL	2.5675 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.42 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.42%

Select Batch:

Data Sheet (272 KB) SDS (393 KB)

COA (248 KB) RP-HPLC (245 KB)

Handling Instructions (2659 KB)

References

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

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5675 mL	12.8373 mL	25.6746 mL	64.1865 mL
	5 mM	0.5135 mL	2.5675 mL	5.1349 mL	12.8373 mL
	10 mM	0.2567 mL	1.2837 mL	2.5675 mL	6.4187 mL
	15 mM	0.1712 mL	0.8558 mL	1.7116 mL	4.2791 mL
	20 mM	0.1284 mL	0.6419 mL	1.2837 mL	3.2093 mL
	25 mM	0.1027 mL	0.5135 mL	1.0270 mL	2.5675 mL
	30 mM	0.0856 mL	0.4279 mL	0.8558 mL	2.1396 mL
	40 mM	0.0642 mL	0.3209 mL	0.6419 mL	1.6047 mL
	50 mM	0.0513 mL	0.2567 mL	0.5135 mL	1.2837 mL
	60 mM	0.0428 mL	0.2140 mL	0.4279 mL	1.0698 mL
	80 mM	0.0321 mL	0.1605 mL	0.3209 mL	0.8023 mL
	100 mM	0.0257 mL	0.1284 mL	0.2567 mL	0.6419 mL

R-IMPP Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

R-IMPP2133832-83-2PF-00932239PF00932239PF 00932239PCSK9Proprotein convertase subtilisin/kexin type 9Inhibitorinhibitorinhibit

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R-IMPP (Synonyms: PF-00932239)

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Complete Stock Solution Preparation Table

R-IMPP Related Classifications

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