PXS-6302 hydrochloride

• CAT Number: I040694
• CAS Number: 2584947-79-3
• Molecular Formula: C10H11ClF3NO2S
• Molecular Weight: 301.71
• Purity: ≥95%
• Synonyms: (Z)-4-(benzenesulfonyl)-3,4,4-trifluorobut-2-en-1-amine;hydrochloride
• InChI: InChI=1S/C10H10F3NO2S.ClH/c11-9(6-7-14)10(12,13)17(15,16)8-4-2-1-3-5-8;/h1-6H,7,14H2;1H/b9-6-
• InChIKey: UOENLHPLNJYJTC-BORNJIKYSA-N
• SMILES: C1=CC=C(C=C1)S(=O)(=O)C(C(=CCN)F)(F)F.Cl

PXS-6302 hydrochloride is an irreversible lysyl oxidase inhibitor with IC50s of 3.7 μM (Bovine LOX), 3.4 μM (rh LOXL1), 0.4 μM (rh LOXL2), 1.5 μM (rh LOXL3), 0.3 μM (rh LOXL4), respectively. PXS-6302 hydrochloride has readily skin penetrability, reduces collagen deposition and significantly improves scar appearance[1].
PXS-6302 hydrochloride demonstrates high permeability to across a monolayer of cells, such as Caco-2 or MDCKII cells[1].
PXS-6302 hydrochloride inhibits LOX, reduces crosslinking and improves scar appearance in porcine models of excisional and burn injury[1].
PXS-6302 hydrochloride (1.5%, oil in water cream; 500 mg cream applied to 16 cm2; external application; once daily, for 28 days) reduces collagen deposition and cross-linkin in murine models of injury and fibrosis under topical application[1].
PXS-6302 hydrochloride (0.5, 1.5, or 3%, oil in water cream; 400 mg cream applied to 16 cm2; external application; once daily, for 12 weeks) also significantly improves scar appearance without reducing tissue strength in porcine injury models under topical application[1].

Reference

[1]. Chaudhari N, et al. Topical application of an irreversible small molecule inhibitor of lysyl oxidases ameliorates skin scarring and fibrosis. Nat Commun. 2022 Sep 22;13(1):5555.
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