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PXS-4681A

Catalog No. T38966 CAS 1478364-87-2

PXS-4681A is a powerful, specific, and irreversible inhibitor of semicarbazide-sensitive amine oxidase (SSAO; VAP-1), with an oral activity and a Ki value of 37 nM. It exhibits exceptional selectivity towards related amine oxidases, ion channels, and seven-transmembrane domain receptors. Additionally, PXS-4681A demonstrates potent anti-inflammatory properties.

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PXS-4681A, CAS 1478364-87-2

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5 mg	Inquiry	$ 970.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	PXS-4681A is a powerful, specific, and irreversible inhibitor of semicarbazide-sensitive amine oxidase (SSAO; VAP-1), with an oral activity and a Ki value of 37 nM. It exhibits exceptional selectivity towards related amine oxidases, ion channels, and seven-transmembrane domain receptors. Additionally, PXS-4681A demonstrates potent anti-inflammatory properties.
Targets&IC50	SSAO:37 nM (Ki)
In vitro	PXS-4681A effectively inhibits the enzyme SSAO/VAP-1 across multiple species including humans, rats, mice, rabbits, and dogs, demonstrating potent activity with IC50 values of 3 nM, 3 nM, 2 nM, 9 nM, and 3 nM, respectively[1].
In vivo	PXS-4681A (2 mg/kg; PO; single dose) effectively reduces neutrophil migration, tumor necrosis factor-α, and interleukin-6 levels in mouse models of both lung and localized inflammation[1]. Demonstrating excellent absorption, bioavailability, and oral half-life, PXS-4681A shows promise in rats at a 10 mg/kg intravenous dose and a 20 mg/kg oral dose. Similarly, in BALB/C mice, the compound maintains these pharmacokinetic attributes at a 2 mg/kg dosage for both administration routes[1]. In an animal model using Carrageenan-induced skin inflammation, a single oral dose of 2 mg/kg significantly lowered local inflammation, notably decreasing exudate volume by 25%[1].

Molecular Weight	296.74
Formula	C10H14ClFN2O3S
CAS No.	1478364-87-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Jonathan S Foot, et al. PXS-4681A, a potent and selective mechanism-based inhibitor of SSAO/VAP-1 with anti-inflammatory effects in vivo. J Pharmacol Exp Ther. 2013 Nov;347(2):365-74.

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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

PXS-4681A 1478364-87-2 PXS 4681A PXS4681A inhibitor inhibit

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