R-IMPP
Based on 1 Customer Validation
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.
- Purity: 99.93%
- CAS No.: 2133832-83-2
- Formula: C24H27N3O2
- Molecular Weight:389.49
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Metabolism/Protease Compound Library
HY-L012
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Anti-Cancer Compound Library
HY-L025
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Anti-Cardiovascular Disease Compound Library
HY-L046
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Heterocyclic Compound Library
HY-L138
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
IC50: 4.8 μM (PCSK9)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Bone marrow cell | IC50 |
>20 μM
Compound: 1; PF-00932239
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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
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[PMID: 29878763] |
| CHO-K1 | IC50 |
<10 μM
Compound: 1; R-IMPP, PF-00932239
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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
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[PMID: 30448414] |
| CHO-K1 | IC50 |
>10 μM
Compound: 1; R-IMPP, PF-00932239
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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
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[PMID: 30448414] |
| CHO-K1 | IC50 |
>10 μM
Compound: 1; R-IMPP, PF-00932239
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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
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[PMID: 30448414] |
| CHO-K1 | IC50 |
4.8 μM
Compound: 1; R-IMPP, PF-00932239
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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
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[PMID: 30448414] |
| CHO-K1 | IC50 |
4.8 μM
Compound: Fig 8, Cpd 80S
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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
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[PMID: 31673315] |
| HeLa | IC50 |
8.04 μM
Compound: 1; PF-00932239
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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
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[PMID: 30482620] |
| Huh-7 | IC50 |
2.2 μM
Compound: 13; R-IMPP
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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
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[PMID: 29519739] |
| Huh-7 | IC50 |
2.63 μM
Compound: 1; PF-00932239
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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
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[PMID: 29878763] |
| 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
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[PMID: 30482620] |
| 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
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[PMID: 29878763] |
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.
Chemical Information
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CAS No. 2133832-83-2
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Appearance Solid
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Molecular Weight 389.49
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Formula C24H27N3O2
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Color Light yellow to yellow
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SMILES
O=C(N(C1=NC=CC2=C1C=CC=C2)[C@H]3CNCCC3)CCC4=CC=C(OC)C=C4
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Synonyms
PF-00932239
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
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.
| 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 |
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