1. Neuronal Signaling
  2. Monoamine Oxidase
  3. PXS-5120A

PXS-5120A 

Cat. No.: HY-130242
Handling Instructions

PXS-5120A is a potent, irreversible fluoroallylamine inhibitor of Lysyl Oxidase-like 2/3 (LOXL2/3) with anti-fibrotic activity. PXS-5120A is >300-fold selective for LOXL2 (Ki of 83 nM; pIC50 of 8.4) over LOXL (pIC50 of 5.8).

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

PXS-5120A Chemical Structure

PXS-5120A Chemical Structure

CAS No. : 2125955-70-4

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Description

PXS-5120A is a potent, irreversible fluoroallylamine inhibitor of Lysyl Oxidase-like 2/3 (LOXL2/3) with anti-fibrotic activity. PXS-5120A is >300-fold selective for LOXL2 (Ki of 83 nM; pIC50 of 8.4) over LOXL (pIC50 of 5.8)[1].

IC50 & Target

pKi: 8.4 (Lysyl Oxidase-like 2) and 5.8 (Lysyl Oxidase-like); Ki: 83 nM (Lysyl Oxidase-like 2)[1]

In Vitro

PXS-5120A (Compound 12k) is a potent inhibitor of the LOXL2/3 enzyme and a moderate blocker of LOXL4. PXS-5120A inhibits recombinant human LOXL2, human fibroblast LOXL2, recombinant mouse LOXL2, recombinant rat LOXL2, collagen oxidation assay, recombinant human LOXL3 and recombinant human LOXL4 with IC50s of 5 nM, 9 nM, 6 nM, 6 nM, 13 nM, 16 nM and 280 nM, respectively.

In Vivo

PXS-5129A is readily absorbed following oral gavage, and once in the circulation, rapidly hydrolyzed to release PXS-5120 (free base) in vivo, affording plasma concentrations well above the LOXL2 IC50 (6 nM) for a prolonged period (>6 h) in mice, while remaining well below the IC50 for LOX throughout[1].

Molecular Weight

481.97

Formula

C₂₂H₂₅ClFN₃O₄S

CAS No.

2125955-70-4

SMILES

O=C(C1=CC2=C(N(C/C(F)=C/CN)C(C)=C2C3=CC=CC(S(=O)(N(C)C)=O)=C3)C=C1)O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

PXS-5120AMonoamine OxidaseMAOInhibitorinhibitorinhibit

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