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AZD0780

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Catalog No. T64362Cas No. 2455427-91-3
Alias PCSK9-IN-12, EX-A6975

AZD0780 (EX-A6975, PCSK9-IN-12) is an orally active PCSK9 inhibitor with high affinity for PCSK9 (Kd < 200 nM). It binds to a specific pocket in the C-terminal domain of PCSK9 without affecting the PCSK9–LDLR interaction. AZD0780 blocks the lysosomal trafficking of the PCSK9–LDLR complex and prevents PCSK9-induced LDLR degradation, making it useful for studies related to hypercholesterolemia.

AZD0780

AZD0780

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Purity: 99.74%
Catalog No. T64362Alias PCSK9-IN-12, EX-A6975Cas No. 2455427-91-3
AZD0780 (EX-A6975, PCSK9-IN-12) is an orally active PCSK9 inhibitor with high affinity for PCSK9 (Kd < 200 nM). It binds to a specific pocket in the C-terminal domain of PCSK9 without affecting the PCSK9–LDLR interaction. AZD0780 blocks the lysosomal trafficking of the PCSK9–LDLR complex and prevents PCSK9-induced LDLR degradation, making it useful for studies related to hypercholesterolemia.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$66In StockIn Stock
5 mg$158In StockIn Stock
10 mg$248In StockIn Stock
25 mg$397In StockIn Stock
50 mg$569In StockIn Stock
100 mg$786In StockIn Stock
200 mg$1,090-In Stock
1 mL x 10 mM (in DMSO)$176In StockIn 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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Batch Information

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Purity:99.74%
Appearance:Solid
Color:White to Yellow
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Product Introduction

Bioactivity
Description
AZD0780 (EX-A6975, PCSK9-IN-12) is an orally active PCSK9 inhibitor with high affinity for PCSK9 (Kd < 200 nM). It binds to a specific pocket in the C-terminal domain of PCSK9 without affecting the PCSK9–LDLR interaction. AZD0780 blocks the lysosomal trafficking of the PCSK9–LDLR complex and prevents PCSK9-induced LDLR degradation, making it useful for studies related to hypercholesterolemia.
Targets&IC50
PCSK9:< 200 nM (Kd)
SynonymsPCSK9-IN-12, EX-A6975
Chemical Properties
Molecular Weight414.41
FormulaC20H20F2N6O2
Cas No.2455427-91-3
SmilesFC(F)Oc1cnc(N[C@H]2CC[C@@H](C2)Nc2ccc(cn2)-n2ccccc2=O)nc1
Relative Density.1.434 g/cm3 (Predicted)
Storage & Solubility Information
Storagekeep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 247.5 mg/mL (597.23 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (7.96 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
1mg5mg10mg50mg
1 mM2.4131 mL12.0653 mL24.1307 mL120.6535 mL
5 mM0.4826 mL2.4131 mL4.8261 mL24.1307 mL
10 mM0.2413 mL1.2065 mL2.4131 mL12.0653 mL
20 mM0.1207 mL0.6033 mL1.2065 mL6.0327 mL
50 mM0.0483 mL0.2413 mL0.4826 mL2.4131 mL
100 mM0.0241 mL0.1207 mL0.2413 mL1.2065 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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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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