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PCSK9-IN-11
🥰Excellent
Catalog No. T67776
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
🥰Excellent
Purity: 99.1%
Catalog No. T67776
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 | Availability | Quantity |
|---|---|---|---|
| 5 mg | $47 | In Stock | |
| 10 mg | $80 | In Stock | |
| 25 mg | $163 | In Stock | |
| 50 mg | $263 | In Stock | |
| 100 mg | $411 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $72 | In Stock |
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Purity:99.1%
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Product Introduction
Bioactivity
Chemical Properties
| 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 | 381.79 |
| Formula | C16H17ClFN5O3 |
| Smiles | CN1C(=O)C2=C(N=C(NCCO)N2CC2=C(F)C(Cl)=CC=C2)N(C)C1=O |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | 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 mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
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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
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