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PXS-5153A

Chemical Structure : PXS-5153A

CAS No.: 2125956-82-1

PXS-5153A (PXS5153A;PXS 5153A)

Catalog No.: PC-35895Not For Human Use, Lab Use Only.

PXS-5153A (PXS5153A) is a potent, selective, fast-acting, dual LOXL2/LOXL3 inhibitor with IC50 of <40 nM against all mammalian species LOXL2, inhibits human LOXL3 with IC50 of 63 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

PXS-5153A (PXS5153A) is a potent, selective, fast-acting, dual LOXL2/LOXL3 inhibitor with IC50 of <40 nM against all mammalian species LOXL2, inhibits human LOXL3 with IC50 of 63 nM.
PXS-5153A displays >40-fold selectivity for LOXL2 over both LOX and LOXL1 and >700-fold over other related amine oxidases.
PXS-5153A dose-dependently reduced LOXL2-mediated collagen oxidation and collagen crosslinking in vitro.
PXS-5153A reduced disease severity and improved liver function by diminishing collagen content and collagen crosslinks in carbon tetrachloride or streptozotocin/high fat diet-induced liver fibrosis models.

Physicochemical Properties

M.Wt 475.404
Formula C20H25Cl2FN4O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(Z)-3-(1-(4-amino-2-fluorobut-2-en-1-yl)-2-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-N,N-dimethylbenzenesulfonamide dihydrochloride

References

1. Schilter H, et al. J Cell Mol Med. 2018 Dec 9. doi: 10.1111/jcmm.14074.

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