Bioactivity | 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]. |
Invitro | PXS-6302 hydrochloride 对单层细胞 (例如 Caco-2 或 MDCKII 细胞) 具有高渗透性[1]。 0 --> PXS-6302 hydrochloride 相关抗体: |
In Vivo | PXS-6302 hydrochloride 在猪切除和烧伤模型中抑制 LOX、减少交联并改善疤痕外观[1]。PXS-6302 hydrochloride (1.5%,水包油乳膏;500 mg 乳膏涂于 16 cm2;外用;每天一次,持续 28 天) 减少小鼠损伤模型中的胶原蛋白沉积和交联蛋白 局部应用下的纤维化[1]。PXS-6302 hydrochloride (0.5、1.5 或 3%,水包油霜;400 mg 霜,涂于 16 cm2;外用;每日一次,持续 12 周) 也可显着改善疤痕外观,且不会减少疤痕局部应用下猪损伤模型的组织强度[1]。 Animal Model: |
Name | PXS-6302 hydrochloride |
CAS | 2584947-79-3 |
Formula | C10H11ClF3NO2S |
Molar Mass | 301.71 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
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. |