PXS-6302 是不可逆的赖氨酸氧化酶 (LOX) 抑制剂，对Bovine LOX、rh LOXL1、rh LOXL2、rh LOXL3、rh LOXL4的IC50分别为 3.7 μM，3.4 μM，0.4 μM，1.5 μM和0.3 μM。PXS-6302 可以轻松渗透皮肤，减少胶原蛋白沉积和交联，显着改善疤痕外观而不降低组织强度。 PXS-6302 在其他纤维化疾病中也可能有更广泛的应用。

PXS-6302 is an irreversible inhibitor of lysyl oxidase with IC50s of 3.7 μM for Bovine LOX, 3.4 μM for rh LOXL1, 0.4 μM for rh LOXL2, 1.5 μM for rh LOXL3, 0.3 μM for rh LOXL4, respectively. PXS-6302 can readily penetrate the skin, reduces collagen deposition and cross-linking, and significantly improves scar appearance without reducing tissue strength. PXS-6302 also has potentially broader applications in other fibrotic diseases.

PXS-6302 exhibits high permeability to across a monolayer of cells, for example, Caco-2 or MDCKII cells [1].

Topical treatment with PXS-6302 inhibits LOX, reduces crosslinking, and improves scar appearance in excisional and burn injury porcine models [1]. PXS-6302 (1.5%, oil in water cream; 500 mg cream applied to 16 cm 2; external application; once daily, for 28 days) reduces collagen deposition and cross-linkin in a topically applied murine model of injury and fibrosis [1]. PXS-6302 (0.5, 1.5, or 3%, oil in water cream; 400 mg cream applied to 16 cm 2; external application; once daily, for 12 weeks) also significantly improves scar appearance without reducing tissue strength in porcine injury models when applied topically [1]. Animal Model: Porcine excision injury model (female Juvenile pigs, 18-20 kg) [1] Dosage: 0.5, 1.5, or 3%, oil in water cream; 400 mg cream applied to 16 cm 2 Administration: External application; 1, 2 and 3 weeks post-injury; once dayly, for 12 weeks Result: Exhibited significantly higher scores for the 3% treated scars indicating significant improvement in scar appearance.

2584947-54-4

C10H10F3NO2S

265.25

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years