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PXS-5120A is an irreversible fluoroallylamine Lysyl Oxidase-like 2/3 (LOXL2/3) inhibitor with anti-fibrotic activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $228 | In Stock | |
2 mg | $325 | In Stock | |
5 mg | $513 | In Stock | |
10 mg | $679 | In Stock | |
25 mg | $993 | In Stock | |
50 mg | $1,360 | In Stock | |
100 mg | $1,820 | In Stock | |
1 mL x 10 mM (in DMSO) | $558 | In Stock |
Description | PXS-5120A is an irreversible fluoroallylamine Lysyl Oxidase-like 2/3 (LOXL2/3) inhibitor with anti-fibrotic activity. |
Targets&IC50 | LOXL2:8.4 (pki), LOXL2:83 nM (ki), LOXL:5.8 (pki) |
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]. |
Molecular Weight | 481.97 |
Formula | C22H25ClFN3O4S |
Cas No. | 2125955-70-4 |
Smiles | Cl.CN(C)S(=O)(=O)c1cccc(c1)-c1c(C)n(C\C(F)=C\CN)c2ccc(cc12)C(O)=O |
Relative Density. | 1.31g/cm3 |
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) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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