Name | PXS-5120A |
Description | PXS-5120A is an irreversible fluoroallylamine Lysyl Oxidase-like 2/3 (LOXL2/3) inhibitor with anti-fibrotic activity. |
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]. |
Storage | Powder: -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)
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Keywords | inhibit | MAO | Monoamine Oxidase | Inhibitor | PXS-5120A | PXS5120A | PXS 5120A |
Inhibitors Related | Norharmane | J-147 | Azure B | Iproniazid Phosphate | Paeonol | Isatin | Methylene Blue | Pargyline hydrochloride | Methylene Blue trihydrate | Phenelzine sulfate | Pargyline | Bifemelane hydrochloride |
Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Neuronal Signaling Compound Library | Antidepressant Compound Library | Inhibitor Library | Mitochondria-Targeted Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |