1. Metabolic Enzyme/Protease
    Neuronal Signaling
  2. FAAH
    MAGL
  3. SA57

SA57 

Cat. No.: HY-103463 Purity: >99.0%
Handling Instructions

SA57 is a potent, selective FAAH inhibitor with IC50s of 3.2 nM and 1.9 nM for mouse and human FAAH. SA57 also inhibits the 2-arachidonoylglycerol hydrolases MAGL (IC50s of 410 nM and 1.4 μM for mouse and human MAGL) and mouse α/β-hydrolase domain-containing protein 6 (mABHD6; IC50 of 850 nM), but not other brain serine hydrolases.

For research use only. We do not sell to patients.

SA57 Chemical Structure

SA57 Chemical Structure

CAS No. : 1346169-63-8

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Description

SA57 is a potent, selective FAAH inhibitor with IC50s of 3.2 nM and 1.9 nM for mouse and human FAAH. SA57 also inhibits the 2-arachidonoylglycerol hydrolases MAGL (IC50s of 410 nM and 1.4 μM for mouse and human MAGL) and mouse α/β-hydrolase domain-containing protein 6 (mABHD6; IC50 of 850 nM), but not other brain serine hydrolases[1][2].

IC50 & Target

IC50: 3.2 nM (Mouse FAAH) and 1.9 nM (Human FAAH); 410 nM (Mouse MAGL) and 1.4 μM (Human MAGL); 850 nM (Mouse ABHD6)[1]

In Vitro

O-Aryl carbamate and N-aryl urea inhibitors have been shown to irreversibly inhibit FAAH by carbamylation of the enzyme’s serine nucleophile. SA57 exhibits clear time-dependent inhibition of FAAH and MAGL, suggesting a covalent mechanism of inactivation, presumably through carbamylation of the active site serine nucleophiles of these enzymes[1].

In Vivo

SA57 (0.01-12.5 mg/kg; intraperitoneal injection; for 2 hours; C57Bl/6 mice) treatment shows distinct dose-responsive activity against brain serine hydrolases (FAAH, MAGL and ABHD6) in vivo[1].

Animal Model: C57Bl/6 mice[1]
Dosage: 0.01 mg/kg, 0.05 mg/kg, 0.25 mg/kg, 1.25 mg/kg, 6.25 mg/kg, 12.5 mg/kg
Administration: Intraperitoneal injection; for 2 hours
Result: Showed distinct dose-responsive activity against brain serine hydrolases. Inhibited FAAH, MAGL and ABHD6 in vivo.
Molecular Weight

338.83

Formula

C₁₇H₂₃ClN₂O₃

CAS No.

1346169-63-8

SMILES

O=C(N1CCC(CCC2=CC=C(Cl)C=C2)CC1)OCC(NC)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >99.0%

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Keywords:

SA57SA 57SA-57FAAHMAGLFatty acid amide hydrolaseMonoacylglycerol lipaseBrainserinehydrolasesABHD6nervousendocannabinoidInhibitorinhibitorinhibit

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