PXS-5120A|2125955-70-4|-陌孚医药/Medlife

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PXS-5120A

目录号: PL07464 纯度: ≥98%

CAS No. :2125955-70-4

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中文名称	PXS-5120A
英文名称	PXS-5120A
英文别名	1H-Indole-5-carboxylic acid, 1-[(2Z)-4-amino-2-fluoro-2-buten-1-yl]-3-[3-[(dimethylamino)sulfonyl]phenyl]-2-methyl-, hydrochloride;BDBM50505638;1-[(Z)-4-amino-2-fluorobut-2-enyl]-3-[3-(dimethylsulfamoyl)phenyl]-2-methylindole-5-carboxylic acid;hydrochloride;CID 130302628;Pxs-5120a hcl
Cas No.	2125955-70-4
分子式	C₂₂H₂₅ClFN₃O₄S
分子量	481.97
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	PXS-5120A 是一种有效的，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。与 LOXL (pIC₅₀ 为 5.8) 相比，PXS-5120A 对 LOXL2 (K_i 为 83 nM; pIC₅₀ 为 8.4) 的选择性高 300 倍以上。
生物活性	PXS-5120A is a potent, irreversible fluoroallylamine inhibitor of Lysyl Oxidase-like 2/3 (LOXL2/3) with anti-fibrotic activity. PXS-5120A is >300-fold selective for LOXL2 (K i of 83 nM; pIC 50 of 8.4) over LOXL (pIC 50 of 5.8).
性状	Solid
IC50 & Target[1][2]	pKi: 8.4 (Lysyl Oxidase-like 2) and 5.8 (Lysyl Oxidase-like); Ki: 83 nM (Lysyl Oxidase-like 2)
体外研究(In Vitro)	PXS-5120A (Compound 12k) is a potent inhibitor of the LOXL2/3 enzyme and a moderate blocker of LOXL4. 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 with IC50s of 5 nM, 9 nM, 6 nM, 6 nM, 13 nM, 16 nM and 280 nM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	PXS-5129A is readily absorbed following oral gavage, and once in the circulation, rapidly hydrolyzed to release PXS-5120 (free base) in vivo, affording plasma concentrations well above the LOXL2 IC 50 (6 nM) for a prolonged period (>6 h) in mice, while remaining well below the IC50 for LOX throughout. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Identification and Optimization of Findlay AD, et al. Mechanism-Based Fluoroallylamine Inhibitors of Lysyl Oxidase-like 2/3. J Med Chem. 2019 Nov 14;62(21):9874-9889.

溶解度数据	In Vitro: DMSO : 125 mg/mL (259.35 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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