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2409963-50-2

2409963-50-2 Structure

2409963-50-2 Structure
IdentificationBack Directory
[Name]

2-Buten-1-amine, 3-fluoro-4-(phenylsulfonyl)-, (2Z)-
[CAS]

2409963-50-2
[Synonyms]

PXS-4787
2-Buten-1-amine, 3-fluoro-4-(phenylsulfonyl)-, (2Z)-
[Molecular Formula]

C10H12FNO2S
[MOL File]

2409963-50-2.mol
[Molecular Weight]

229.27
Chemical PropertiesBack Directory
[Boiling point ]

423.2±45.0 °C(Predicted)
[density ]

1.250±0.06 g/cm3(Predicted)
[pka]

6.89±0.29(Predicted)
Hazard InformationBack Directory
[Uses]

PXS-4787 is a specific and effective pan-LOX (lysyl oxidase) inhibitor for abolishing lysyl oxidase activity. PXS-4787 inhibits LOX with IC50s of 2 μM (Bovine LOX), 3.2 μM (rh LOXL1), 0.6 μM (rh LOXL2), 1.4 μM (rh LOXL3), 0.2 μM (rh LOXL4), respectively[1].
[in vivo]

PXS-4787 (3%, oil in water cream; 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-4787 (3%, oil in water cream; external application; once daily, for 12 weeks) also significantly improves scar appearance without reducing tissue strength in porcine injury models under topical application[1].

Animal Model:Porcine excision injury model (female Juvenile pigs, 18-20 kg)[1]
Dosage:3%, oil in water cream; 400 mg cream applied to 16 cm2
Administration:External application; 1, 2 and 3 weeks post-injury; once dailly, for 12 weeks
Result:Improved the appearance of scar in relevant in vivo models, indicative of a targetdriven, as opposed to compound-specific, effect.
[References]

[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. DOI:10.1038/s41467-022-33148-5
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