PXS-5153A

PXS-5153A is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC50 of <40 nM for LOXL2 across all mammalian species and an IC50 of 63 nM for human LOXL3. PXS-5153A could reduce crosslinks and ameliorates fibrosis.

Product information

CAS Number: 2125956-82-1

Molecular Weight: 475.41

Formula: C20H25Cl2FN4O2S

Chemical Name: 3-{1-[(2Z)-4-amino-2-fluorobut-2-en-1-yl]-2-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl}-N,N-dimethylbenzene-1-sulfonamide dihydrochloride

Smiles: Cl.Cl.CN(C)S(=O)(=O)C1=CC(=CC=C1)C1C2N=CC=CC=2N(C/C(/F)=C/CN)C=1C

InChiKey: INSNGJNTNAUITD-ULPVBNQHSA-N

InChi: InChI=1S/C20H23FN4O2S.2ClH/c1-14-19(15-6-4-7-17(12-15)28(26,27)24(2)3)20-18(8-5-11-23-20)25(14)13-16(21)9-10-22;;/h4-9,11-12H,10,13,22H2,1-3H3;2*1H/b16-9-;;

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

PXS-5153A exhibits an IC50 of <40 nM for LOXL2 across all mammalian species tested. PXS-5153A also inhibits human LOXL3 with an IC50 value of 63 nM. PXS-5153A is >40-fold selective for LOXL2 over both LOX and LOXL1 and >700-fold selective over other related amine oxidases. PXS-5153A is a fast acting inhibitor, with enzymatic activity almost entirely blocked within 15 minutes .

In Vivo:

As expected, rhLOXL2 dose-dependently induce oxidation of collagen with PXS-5153A dose-dependently impeding collagen oxidation. Therapeutic treatment of PXS-5153A substantially reduces immature crosslink formation compared with the CCl4 treated animals. Mature crosslink formation is also reduced by PXS-5153A treatment. All groups with therapeutic treatment of PXS-5153A show a significant reduction in DHLNL formation compared to the CCl4 treated animals. Treatment with PXS-5153A causes a significantly reduction in HYP compared to the CCl4 group. In addition, the amount of fibrillar collagen is markedly augmented by disease as seen by the 2.2-fold increase in percentage coverage area by Picrosirius red staining, which is reduced by PXS-5153A.

Products are for research use only. Not for human use.