PXS-5153A 是一种有效、特异性和速效的Lysyl Oxidase-like 2/3 (LOXL2/3) 抑制剂,其酶活性在 15 分钟内几乎完全阻断。 PXS-5153A 可以减少交联并改善纤维化。
半岛bd体育手机客户端 描述
PXS-5153A is an effective, selective, and fast-acting inhibitor of lysyl oxidase like 2/3 enzymes with enzymatic activity almost entirely blocked within 15 minutes. PXS-5153A could reduce crosslinks and ameliorates fibrosis.
体外活性
PXS-5153A is >40-fold selective for LOXL2 over both LOX and LOXL1 and >700-fold selective over other related amine oxidases. PXS-5153A exhibits an IC50 of<40 nM for LOXL2 across all mammalian species tested. PXS-5153A also inhibits human LOXL3 with an IC50 value of 63 nM[1].
体内活性
rhLOXL2 dose-dependently induces oxidation of collagen with PXS-5153A dose-dependently impeding collagen oxidation. Therapeutic treatment of PXS-5153A substantially reduces immature crosslink formation compared with the CCl4 treated animals. Mature crosslink formation is also reduced by PXS-5153A treatment. All groups with therapeutic treatment of PXS-5153A show a significant reduction in DHLNL formation and HYP compared to the CCl4 treated animals[1].
Cas No.
2125956-82-1
分子式
C20H25Cl2FN4O2S
分子量
475.41
储存和溶解度
DMSO:20mg/mL
H2O:20mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years