PXS-5120A |cas 2125955-70-4|DC Chemicals

Cas No.:	2125955-70-4
Chemical Name:	PXS-5120A
Synonyms:	1H-Indole-5-carboxylic acid, 1-[(2Z)-4-amino-2-fluoro-2-buten-1-yl]-3-[3-[(dimethylamino)sulfonyl]phenyl]-2-methyl-, hydrochloride
SMILES:	C1(=C(C)N(C/C(=C/CN)/F)C2C=CC(=CC1=2)C(O)=O)C1C=CC=C(S(=O)(N(C)C)=O)C=1.Cl
Formula:	C₂₂H₂₅ClFN₃O₄S
M.Wt:	481.97
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO

Description:	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 (Ki of 83 nM; pIC50 of 8.4) over LOXL (pIC50 of 5.8)[1].
Target:	pKi: 8.4 (Lysyl Oxidase-like 2) and 5.8 (Lysyl Oxidase-like); Ki: 83 nM (Lysyl Oxidase-like 2)[1]
In Vivo:	PXS-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 IC50 (6 nM) for a prolonged period (>6 h) in mice, while remaining well below the IC50 for LOX throughout[1].
In Vitro:	PXS-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 IC50s of 5 nM, 9 nM, 6 nM, 6 nM, 13 nM, 16 nM and 280 nM, respectively.
References:	[1]. Identification and Optimization of Findlay AD, et al. Mechanism-Based Fluoroallylamine Inhibitors of Lysyl Oxidase-like 2/3. J Med Chem. 2019 Nov 14;62(21):9874-9889.

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