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AA26-9 is a potent and broad spectrum serine hydrolase inhibitor. AA26-9-inhibited enzymes originated from diverse functional subclasses of serine hydrolases, including lipases/phospholipases (AADACL1, ABHD6, ESD, FAAH, PAFAH2, LYPLA3), peptidases (APEH, PRCP, CTSA), thioesterases (LYPLA1, LYPLA2), and uncharacterized enzymes (ABHD11, ABHD13, BAT5). AA26-9 inhibits one of its enzyme targets LYPLA1 by covalent carbamoylation of the enzyme’s serine nucleophile (S114). AA26-9 inhibits 1/3 of the over 40 serine hydrolase found in T-cells.
J Pharm Sci. 2021 Sep;110(9):3313-3323.
Polysorbate degradation and particle formation in a high concentration mAb: formulation strategies to minimize effect of enzymatic polysorbate degradation
AA26-9 purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | T-cell hybridoma cells |
| Preparation method | Cells were then lysed and analyzed by competitive ABPP with the FP-Rh probe. Gel-based ABPP detected SHs that were inhibited by both AA38-3 and AA26-9, as well as a substantial number of additional SHs that were only inhibited by the triazole AA26-9. |
| Concentrations | 20 μM |
| Incubation time | 4 h |
| Animal Experiment | |
|---|---|
| Animal models | Mice |
| Formulation | PEG300 or 18:1:1 saline/ethanol/emulphor intraperitoneally |
| Dosages | 0.2–1.6 mg/kg |
| Administration | |
| Molecular Weight | 166.18 |
| Formula | C7H10N4O |
| CAS Number | 1312782-34-5 |
| Solubility (25°C) | Water ≥ 80 mg/mL DMSO 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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