1. Neuronal Signaling
  2. Monoamine Oxidase
  3. PXS-4681A

PXS-4681A 

Cat. No.: HY-117833
Handling Instructions

PXS-4681A is a potent, selective, irreversible and orally active semicarbazide-sensitive amine oxidase (SSAO; VAP-1) inhibitor with a Ki of 37 nM. PXS-4681A shows highly selectivity over related amine oxidases, ion channels, and seven-transmembrane domain receptors. PXS-4681A has anti-inflammatory effects.

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

PXS-4681A Chemical Structure

PXS-4681A Chemical Structure

CAS No. : 1478364-87-2

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Description

PXS-4681A is a potent, selective, irreversible and orally active semicarbazide-sensitive amine oxidase (SSAO; VAP-1) inhibitor with a Ki of 37 nM. PXS-4681A shows highly selectivity over related amine oxidases, ion channels, and seven-transmembrane domain receptors. PXS-4681A has anti-inflammatory effects[1].

IC50 & Target

Ki: 37 nM (SSAO)[1]

In Vitro

PXS-4681A is an inhibitor of SSAO/VAP-1 in human, rat, mouse, rabbit, and dog species with IC50 values of 3 nM, 3 nM, 2 nM, 9 nM and 3nM, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PXS-4681A (2 mg/kg; PO; single dose) attenuates neutrophil migration, tumor necrosis factor-α, and interleukin-6 levels in mouse models of lung inflammation and localized inflammation[1].
In rats, PXS-4681A is well absorbed with good bioavailability and oral half-life at the 10 mg/kg i.v. dose and the 20 mg/kg PO dose. Similarly, in BALB/C mice, PXS-4681A is well absorbed with good bioavailability and oral half-life at 2 mg/kg in both intravenous and oral studies[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Carrageenan-induced skin inflammation mice[1]
Dosage: 2 mg/kg
Administration: oral administration; single dose
Result: Reduced local inflammation, causing a significant reduction in exudate volume by 25%.
Molecular Weight

296.75

Formula

C₁₀H₁₄ClFN₂O₃S

CAS No.
SMILES

O=S(C1=CC=C(OC/C(CN)=C\F)C=C1)(N)=O.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

PXS-4681AMonoamine OxidaseMAOanti-inflammatorySSAOVAP-1oralInhibitorinhibitorinhibit

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PXS-4681A
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HY-117833
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