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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Phospholipase Products |
|---|
| Phospholipase A2
Phospholipase A2 (PLA2) catalyzes the hydrolysis of the sn-2 position of membrane glycerophospholipids to liberate arachidonic acid (AA). |
| Melittin
Melittin is a PLA2 activator that stimulates the activity of low molecular weight PLA2 without increasing the activity of high molecular weight PLA2. |
| trans-4-phenylbut-3-en-2-one
trans-Benzylideneacetone (trans-Benzalacetone), a metabolite of gram-negative entomopathogenic bacterium Xenorhabdus nematophila, is an enzyme inhibitor against phospholipase A2 (PLA2). |
| SYN-020
SYN-020 is an orally active recombinant bovine intestinal alkaline phosphatase (IAP) for studies related to digestive disorders. |
| IIAEK
IIAEK is a novel cholesterol-lowering pentapeptide derived from bovine milk β-lactoglobulin that targets intestinal alkaline phosphatase (IAP) and improves cholesterol metabolism through the specific activation of IAP and down-regulation of ABCA1. Sequence: Ile-Ile-Ala-Glu-Lys |
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