Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PXS-4681A is a powerful, specific, and irreversible inhibitor of semicarbazide-sensitive amine oxidase (SSAO; VAP-1), with an oral activity and a Ki value of 37 nM. It exhibits exceptional selectivity towards related amine oxidases, ion channels, and seven-transmembrane domain receptors. Additionally, PXS-4681A demonstrates potent anti-inflammatory properties.
产品描述 | PXS-4681A is a powerful, specific, and irreversible inhibitor of semicarbazide-sensitive amine oxidase (SSAO; VAP-1), with an oral activity and a Ki value of 37 nM. It exhibits exceptional selectivity towards related amine oxidases, ion channels, and seven-transmembrane domain receptors. Additionally, PXS-4681A demonstrates potent anti-inflammatory properties. |
靶点活性 | SSAO:37 nM (Ki) |
体外活性 | PXS-4681A is an inhibitor of SSAO/VAP-1 in human, rat, mouse, rabbit, and dog species with IC 50 values of 3 nM, 3 nM, 2 nM, 9 nM and 3nM, respectively[1]. |
体内活性 | PXS-4681A (2 mg/kg; PO; single dose) attenuates neutrophil migration, tumor necrosis factor-α, and interleukin-6 levels in mouse models of lung inflammation and localized inflammation[1]. In rats, PXS-4681A is well absorbed with good bioavailability and oral half-life at the 10 mg/kg i.v. dose and the 20 mg/kg PO dose. Similarly, in BALB/C mice, PXS-4681A is well absorbed with good bioavailability and oral half-life at 2 mg/kg in both intravenous and oral studies[1]. Animal Model: Carrageenan-induced skin inflammation mice[1]Dosage: 2 mg/kg Administration: oral administration; single dose Result: Reduced local inflammation, causing a significant reduction in exudate volume by 25%. |
分子量 | 296.74 |
分子式 | C10H14ClFN2O3S |
CAS No. | 1478364-87-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
PXS-4681A 1478364-87-2 PXS 4681A PXS4681A Inhibitor inhibitor inhibit