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AA26-9

Cat. No. M6074
AA26-9 Structure
Size Price Availability Quantity
5mg USD 300 In stock
10mg USD 480 In stock
50mg USD 1200 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

AA26-9 is synthesized based on a piperazine scaffold shown previously to inhibit serine hydrolases in the context of p-nitrophenoxy carbamate. 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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 166.18
Formula C7H10N4O
CAS Number 1312782-34-5
Purity >99%
Solubility 10 mM in DMSO
Storage at -20°C
References

Click-generated triazole ureas as ultrapotent in vivo-active serine hydrolase inhibitors.
Adibekian A, et al. Nat Chem Biol. 2011 May 15;7(7):469-78. PMID: 21572424.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AA26-9 supplier, Phospholipase, inhibitors

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