AGG-523 is a selective, reversible inhibitor of the aggrecanases ADAMTS4 and ADAMTS5, demonstrating IC50 values of <0.03 μM and 0.04 μM, respectively. This non-hydroxamate, zinc-binding compound also exhibits inhibitory effects on MMP-2, MMP-8, and MMP-12. AGG-523 has been shown to reduce the release of aggrecanase-generated ARG-aggrecan fragments in synovial fluid and attenuates surgery-induced ARG-aggrecan release in rat joint models. It is an essential compound for studying cartilage degradation and investigating therapies for osteoarthritis.
Fig. 1 · Structure
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AGG-523
ADAMTS4/ADAMTS5 Inhibitor
AGG-523 is a selective, reversible inhibitor of the aggrecanases ADAMTS4 and ADAMTS5, demonstrating IC50 values of <0.03 μM and 0.04 μM, respectively. This non-hydroxamate, zinc-binding compound also exhibits inhibitory effects on MMP-2, MMP-8, and MMP-12. AGG-523 has been shown to reduce the release of aggrecanase-generated ARG-aggrecan fragments in synovial fluid and attenuates surgery-induced ARG-aggrecan release in rat joint models. It is an essential compound for studying cartilage degradation and investigating therapies for osteoarthritis.
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Biological Activity
Specifications
| Manufacturer | Adooq Bioscience |
|---|---|
| Actions | Inhibitor |
| CAS Number | 920289-29-8 |
| Applications | ADAMTS4/ADAMTS5 Inhibitor |
| Formula | C28H29FN2O4 |
| Molecular Weight | 476.54 |
| Synonyms | PF-5212371 |
| SMILES | FC(C=C1)=CC=C1CC(C)(C)NC([C@H](CCC(O)=O)NC(C2=CC=C(C3=CC=CC=C3)C=C2)=O)=O |
Storage & Solubility
In Vitro Solubility
Reported Solubility
No reported solubility data are available for this product.
Preparing Stock Solutions
| Concentration | |
|---|---|
Values use four significant digits. Prepare to the final solution volume; this is not the volume of solvent to add.
Stock preparation is unavailable for this product molecular weight.
Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.
Storage
Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.