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PXS-5120A

Catalog No. T12584Cas No. 2125955-70-4

PXS-5120A is an irreversible fluoroallylamine Lysyl Oxidase-like 2/3 (LOXL2/3) inhibitor with anti-fibrotic activity.

PXS-5120A

PXS-5120A

Purity: 98.36%
Catalog No. T12584Cas No. 2125955-70-4
PXS-5120A is an irreversible fluoroallylamine Lysyl Oxidase-like 2/3 (LOXL2/3) inhibitor with anti-fibrotic activity.
Pack SizePriceAvailabilityQuantity
1 mg$228In Stock
2 mg$325In Stock
5 mg$513In Stock
10 mg$679In Stock
25 mg$993In Stock
50 mg$1,360In Stock
100 mg$1,820In Stock
1 mL x 10 mM (in DMSO)$558In Stock
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Purity:98.36%
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Product Introduction

Bioactivity
Description
PXS-5120A is an irreversible fluoroallylamine Lysyl Oxidase-like 2/3 (LOXL2/3) inhibitor with anti-fibrotic activity.
Targets&IC50
LOXL:5.8 (pki), LOXL2:8.4 (pki), LOXL2:83 nM (ki)
In vitro
PXS-5120A is >300-fold selective for LOXL2 (Ki of 83 nM; pIC50 of 8.4) over LOXL (pIC50 of 5.8)[1]. 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(IC50s of 5 nM, 9 nM, 6 nM, 6 nM, 13 nM, 16 nM and 280 nM, respectively)[1].
In vivo
In mice, PXS-5129A is readily absorbed following oral gavage, and 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), while remaining well below the IC50 for LOX throughout[1].
Chemical Properties
Molecular Weight481.97
FormulaC22H25ClFN3O4S
Cas No.2125955-70-4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (103.74 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0748 mL10.3741 mL20.7482 mL103.7409 mL
5 mM0.4150 mL2.0748 mL4.1496 mL20.7482 mL
10 mM0.2075 mL1.0374 mL2.0748 mL10.3741 mL
20 mM0.1037 mL0.5187 mL1.0374 mL5.1870 mL
50 mM0.0415 mL0.2075 mL0.4150 mL2.0748 mL
100 mM0.0207 mL0.1037 mL0.2075 mL1.0374 mL

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TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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