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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $66 | In Stock | In Stock | |
| 5 mg | $158 | In Stock | In Stock | |
| 10 mg | $248 | In Stock | In Stock | |
| 25 mg | $397 | In Stock | In Stock | |
| 50 mg | $569 | In Stock | In Stock | |
| 100 mg | $786 | In Stock | In Stock | |
| 200 mg | $1,090 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $176 | In Stock | In Stock |
| 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) |
| Synonyms | PCSK9-IN-12, EX-A6975 |
| Molecular Weight | 414.41 |
| Formula | C20H20F2N6O2 |
| Cas No. | 2455427-91-3 |
| Smiles | FC(F)Oc1cnc(N[C@H]2CC[C@@H](C2)Nc2ccc(cn2)-n2ccccc2=O)nc1 |
| Relative Density. | 1.434 g/cm3 (Predicted) |
| Color | Yellow |
| Appearance | Solid |
| 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: 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 recommeded. 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
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