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Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $970 | Backorder |
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. |
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 |
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