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PXS-5120A 是一种不可逆的 Lysyl Oxidase-like 2/3 (LOXL2/3) 的氟代烯丙胺抑制剂,具有抗纤维化活性。
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PXS-5120A 是一种不可逆的 Lysyl Oxidase-like 2/3 (LOXL2/3) 的氟代烯丙胺抑制剂,具有抗纤维化活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 2,320 | 现货 | |
5 mg | ¥ 5,130 | 现货 | |
10 mg | ¥ 6,780 | 现货 | |
25 mg | ¥ 9,870 | 现货 | |
50 mg | ¥ 13,600 | 现货 | |
100 mg | ¥ 18,300 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 5,620 | 现货 |
产品描述 | PXS-5120A is an irreversible fluoroallylamine Lysyl Oxidase-like 2/3 (LOXL2/3) inhibitor with anti-fibrotic activity. |
靶点活性 | LOXL:5.8 (pki), LOXL2:8.4 (pki), LOXL2:83 nM (ki) |
体外活性 | PXS-5120A is >300-fold selective for LOXL2 (Ki of 83 nM; pIC50 of 8.4) over LOXL (pIC50 of 5.8)[1]. PXS-5120A inhibits recombinant human LOXL2, human fibroblast LOXL2, recombinant mouse LOXL2, recombinant rat LOXL2, collagen oxidation assay, recombinant human LOXL3 and recombinant human LOXL4(IC50s of 5 nM, 9 nM, 6 nM, 6 nM, 13 nM, 16 nM and 280 nM, respectively)[1]. |
体内活性 | In mice, PXS-5129A is readily absorbed following oral gavage, and rapidly hydrolyzed to release PXS-5120 (free base) in vivo, affording plasma concentrations well above the LOXL2 IC50 (6 nM) for a prolonged period (>6 h), while remaining well below the IC50 for LOX throughout[1]. |
分子量 | 481.97 |
分子式 | C22H25ClFN3O4S |
CAS No. | 2125955-70-4 |
Smiles | Cl.CN(C)S(=O)(=O)c1cccc(c1)-c1c(C)n(C\C(F)=C\CN)c2ccc(cc12)C(O)=O |
密度 | 1.31g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (103.74 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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