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PCSK9-IN-11
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Catalog No. T67776Cas No. 2882035-56-3
PCSK9-IN-11 (compound 5r) is a potent PCSK9 inhibitor with oral activity, exhibiting inhibitory activity on PCSK9 transcription in HepG2 cells (IC50 = 5.7 μM) and capable of increasing LDL receptor (LDLR) protein levels. PCSK9-IN-11 is applicable for atherosclerosis research.
PCSK9-IN-11
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Purity: 99.10%
Catalog No. T67776Cas No. 2882035-56-3
PCSK9-IN-11 (compound 5r) is a potent PCSK9 inhibitor with oral activity, exhibiting inhibitory activity on PCSK9 transcription in HepG2 cells (IC50 = 5.7 μM) and capable of increasing LDL receptor (LDLR) protein levels. PCSK9-IN-11 is applicable for atherosclerosis research.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $47 | In Stock | In Stock | |
| 10 mg | $80 | In Stock | In Stock | |
| 25 mg | $163 | In Stock | In Stock | |
| 50 mg | $263 | In Stock | In Stock | |
| 100 mg | $411 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $72 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.10%
Appearance:Solid
Color:White
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | PCSK9-IN-11 (compound 5r) is a potent PCSK9 inhibitor with oral activity, exhibiting inhibitory activity on PCSK9 transcription in HepG2 cells (IC50 = 5.7 μM) and capable of increasing LDL receptor (LDLR) protein levels. PCSK9-IN-11 is applicable for atherosclerosis research. |
| In vitro | PCSK9-IN-11 (compound 5r) (0-25 μM, 24 h) significantly reduces PCSK9 protein levels and increases LDLR expression in a dose-dependent manner[1]. |
| In vivo | PCSK9-IN-11 (compound 5r) (0-1000 mg/kg, gavage, once) demonstrates superior safety in vivo, with an LD50 value exceeding 1000 mg/kg. Administered at 30 mg/kg via gavage once daily for 8 weeks, PCSK9-IN-11 significantly inhibits liver PCSK9 expression and slightly reduces serum PCSK9 levels [1]. |
| Molecular Weight | 381.789 |
| Formula | C16H17ClFN5O3 |
| Cas No. | 2882035-56-3 |
| Smiles | O=C1C2=C(N=C(NCCO)N2CC=3C=CC=C(Cl)C3F)N(C(=O)N1C)C |
| Storage | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 3.82 mg/mL (10.01 mM), Sonication is recommended.  | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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Calculator
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, and a total of 10 animals are to be administered, using a formulation of 
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 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 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 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.
Dose Conversion
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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
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