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SA57

Catalog No. T12826 CAS 1346169-63-8

SA57 is a potent, selective inhibitor of FAAH(IC50s of 3.2 nM and 1.9 nM for mouse and human FAAH).

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SA57, CAS 1346169-63-8

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	SA57 is a potent, selective inhibitor of FAAH(IC50s of 3.2 nM and 1.9 nM for mouse and human FAAH).
Targets&IC50	Human FAAH:1.9 nM , Mouse ABHD6:850 nM , mouse MAGL:410 nM , Mouse FAAH:3.2 nM , human MAGL:1.4 μM
In vitro	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	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)[1].

Molecular Weight	338.83
Formula	C17H23ClN2O3
CAS No.	1346169-63-8

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Niphakis MJ, et al. O-hydroxyacetamide carbamates as a highly potent and selective class of endocannabinoid hydrolase inhibitors. ACS Chem Neurosci. 2012 May 16;3(5):418-26. 2. Owens RA, et al. Discriminative Stimulus Properties of the Endocannabinoid Catabolic Enzyme Inhibitor SA-57 in Mice. J Pharmacol Exp Ther. 2016 Aug;358(2):306-14.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

SA57 1346169-63-8 Metabolism Neuroscience FAAH SA-57 Inhibitor inhibitor inhibit

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