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PXS-5153A

    
≥98%

(Z)-3-(1-(4-amino-2-fluorobut-2-en-1-yl)-2-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-N,N-dimethylbenzenesulfonamide dihydrochloride

源叶(MedMol)
S89497 一键复制产品信息
2125956-82-1
C20H25Cl2FN4O2S
475.4044
PXS-5153A; PXS 5153A; PXS5153A; PXS-5153; PXS 5153; PXS5153;
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
S89497-5mg
≥98%

¥2900.00

货期:3-5天 - - - -
S89497-10mg
≥98%

¥4300.00

货期:3-5天 - - - -
S89497-25mg
≥98%

¥6800.00

货期:3-5天 - - - -
S89497-100mg
≥98%

¥12500.00

货期:3-5天 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
产品描述: PXS-5153A is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC50 of <40 nM for LOXL2 across all mammalian species and an IC50 of 63 nM for human LOXL3. PXS-5153A could reduce crosslinks and ameliorates fibrosis
靶点: IC50: <40 nM (LOXL2 across all mammalian species), 63 nM (human LOXL3)
体外研究: 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. PXS-5153A is >40-fold selective for LOXL2 over both LOX and LOXL1 and >700-fold selective over other related amine oxidases. PXS-5153A is a fast acting inhibitor, with enzymatic activity almost entirely blocked within 15 minutes
体内研究: As expected, rhLOXL2 dose-dependently induce 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 compared to the CCl4 treated animals. Treatment with PXS-5153A causes a significantly reduction in HYP compared to the CCl4 group. In addition, the amount of fibrillar collagen is markedly augmented by disease as seen by the 2.2-fold increase in percentage coverage area by Picrosirius red staining, which is reduced by PXS-5153A
参考文献: 1. Schilter H, et al. The lysyl oxidase like 2/3 enzymatic inhibitor, PXS-5153A, reduces crosslinks and ameliorates fibrosis. J Cell Mol Med. 2018 Dec 9.
保存条件: -20℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 2.103 ml 10.517 ml 21.035 ml
5 mM 0.421 ml 2.103 ml 4.207 ml
10 mM 0.21 ml 1.052 ml 2.103 ml
50 mM 0.042 ml 0.21 ml 0.421 ml
注意: 部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。

参考文献

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