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编 号：F752171
分子式：C10H12FNO2S
分子量：229.27
分子式：C10H12FNO2S
分子量：229.27
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CAS No: 2409963-50-2
产品详情
生物活性：
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.
体内研究：
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.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.Animal Model:Porcine excision injury model (female Juvenile pigs, 18-20 kg)
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.
体外研究：
Lysyl oxidases stabilize the main component of scar tissue, collagen, and drive scar stiffness and appearance.PXS-4787 (0-10 μM; 15 min-4 h) dose- and time-dependently inhibits lysyl oxidase and displays comparable inhibitory activity across species.PXS-4787 (0-100 μM; 72 h) is well tolerated by primary human dermal fibroblasts, (10 μM; 11 d) reduces collagen formation, deposition and crosslinking in primary human dermal fibroblasts cultured in vitro.PXS-4787 (10 μM; 48 h) induces differential gene expression in fibroblasts and keratinocytes, including COL1A1, LOX, GAPDH, PGK1.
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.
体内研究：
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.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.Animal Model:Porcine excision injury model (female Juvenile pigs, 18-20 kg)
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.
体外研究：
Lysyl oxidases stabilize the main component of scar tissue, collagen, and drive scar stiffness and appearance.PXS-4787 (0-10 μM; 15 min-4 h) dose- and time-dependently inhibits lysyl oxidase and displays comparable inhibitory activity across species.PXS-4787 (0-100 μM; 72 h) is well tolerated by primary human dermal fibroblasts, (10 μM; 11 d) reduces collagen formation, deposition and crosslinking in primary human dermal fibroblasts cultured in vitro.PXS-4787 (10 μM; 48 h) induces differential gene expression in fibroblasts and keratinocytes, including COL1A1, LOX, GAPDH, PGK1.
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