An affinity probe for NAAA using click chemistry; inhibits the hydrolysis of the NAAA substrate PAMCA in HEK293 cells (IC50s = 6 and 13 nM for human and rat recombinant enzymes

ARN14686 – 10 mg

Brand:
Cayman
CAS:
1628345-10-7
Storage:
-20
UN-No:
Non-Hazardous - /

ARN14686 is an activity-based affinity probe for the detection of N-acylethanolamine acid amidase (NAAA) using click chemistry.{36895} It binds covalently to the N-terminal cysteine of catalytically active NAAA to form a thioester adduct. ARN14686 inhibits the hydrolysis of the NAAA substrate PAMCA in HEK293 cells (IC50s = 6 and 13 nM for human and rat recombinant enzymes, respectively) and is selective for NAAA over acid ceramidase (IC50 = 1,200 nM for the rat enzyme). It labels NAAA in HEK293 cells overexpressing human or rat recombinant NAAA and, when used at concentrations of 1 and 10 µM, in rat lung lysosomal fractions in vitro. It also detects NAAA in lung lysosomal fractions following intravenous administration at a dose of 10 mg/kg in rats. ARN14686 (3 mg/kg) has been used to determine that catalytically active NAAA is present in inflamed rat paw in a complete Freund’s adjuvant model of inflammation.{36896}  

 

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Description

An affinity probe for NAAA using click chemistry; inhibits the hydrolysis of the NAAA substrate PAMCA in HEK293 cells (IC50s = 6 and 13 nM for human and rat recombinant enzymes, respectively); selective for NAAA over acid ceramidase (IC50 = 1,200 nM for the rat enzyme); labels NAAA in HEK293 cells; labels NAAA in rat lung lysosomal fractions in vitro at 1 and 10 µM; detects NAAA in lung lysosomal fractions following a 10 mg/kg, i.v. dose in rats; has been used to determine that catalytically active NAAA is present in inflamed rat paw in a complete Freund’s adjuvant model of inflammation at 3 mg/kg

Formal name: N-[(3S)-2-oxo-3-azetidinyl]-carbamic acid, 10-undecyn-1-yl ester

Synonyms: 

Molecular weight: 280.4

CAS: 1628345-10-7

Purity: ≥98%

Formulation: A crystalline solid

Application|Click Chemistry||Product Type|Biochemicals|Labeling & Detection|Affinity Probes||Research Area|Immunology & Inflammation|Innate Immunity

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