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 ( K i of 83 nM; pIC 50 of 8.4) over LOXL ( pIC 50 of 5.8)In VitroPXS-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 IC 50 s of 5 nM, 9 nM, 6 nM, 6 nM, 13 nM, 16 nM and 280 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoPXS-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 IC 50 (6 nM) for a prolonged period (>6 h) in mice, while remaining well below the IC50 for LOX throughout . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:pKi: 8.4 (Lysyl Oxidase-like 2) and 5.8 (Lysyl Oxidase-like),Ki: 83 nM (Lysyl Oxidase-like 2). Specification: 0.98 Molecular Formula: C22H25ClFN3O4S Molecular Weight: 481.97
- UPC:
- 51111644
- Condition:
- New
- Availability:
- 8-12 weeks
- Weight:
- 1.06 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- P646363-5mg
- CAS:
- 2125955-70-4
- Product Size:
- 5mg
