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.
Product information
CAS Number: 1478364-87-2
Molecular Weight: 296.75
Formula: C10H14ClFN2O3S
Chemical Name: 4-{[(2Z)-2-(aminomethyl)-3-fluoroprop-2-en-1-yl]oxy}benzene-1-sulfonamide hydrochloride
Smiles: Cl.NC/C(/COC1C=CC(=CC=1)S(N)(=O)=O)=C/F
InChiKey: VBGNJMUEMDYZJJ-HGKIGUAWSA-N
InChi: InChI=1S/C10H13FN2O3S.ClH/c11-5-8(6-12)7-16-9-1-3-10(4-2-9)17(13,14)15;/h1-5H,6-7,12H2,(H2,13,14,15);1H/b8-5-;
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
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. 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.
Products are for research use only. Not for human use.
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