Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PXS-6302 是不可逆的赖氨酸氧化酶 (LOX) 抑制剂,对Bovine LOX、rh LOXL1、rh LOXL2、rh LOXL3、rh LOXL4的IC50分别为 3.7 μM,3.4 μM,0.4 μM,1.5 μM 和0.3 μM。PXS-6302 可以轻松渗透皮肤,减少胶原蛋白沉积和交联,显着改善疤痕外观而不降低组织强度。 PXS-6302 在其他纤维化疾病中也可能有更广泛的应用。 在相同实验条件下,摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性,但盐形式 PXS-6302 hydrochloride 的水溶性和稳定性通常比游离态更好。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | 待询 | 6-8周 | ||
50 mg | 待询 | 6-8周 | ||
100 mg | 待询 | 6-8周 |
PXS-6302 的其他形式现货产品:
产品描述 | PXS-6302 is an irreversible inhibitor of lysyl oxidase with IC50s of 3.7 μM for Bovine LOX, 3.4 μM for rh LOXL1, 0.4 μM for rh LOXL2, 1.5 μM for rh LOXL3, 0.3 μM for rh LOXL4, respectively. PXS-6302 can readily penetrate the skin, reduces collagen deposition and cross-linking, and significantly improves scar appearance without reducing tissue strength. PXS-6302 also has potentially broader applications in other fibrotic diseases. |
体外活性 | PXS-6302 exhibits high permeability to across a monolayer of cells, for example, Caco-2 or MDCKII cells [1]. |
体内活性 | Topical treatment with PXS-6302 inhibits LOX, reduces crosslinking, and improves scar appearance in excisional and burn injury porcine models [1]. PXS-6302 (1.5%, oil in water cream; 500 mg cream applied to 16 cm 2; external application; once daily, for 28 days) reduces collagen deposition and cross-linkin in a topically applied murine model of injury and fibrosis [1]. PXS-6302 (0.5, 1.5, or 3%, oil in water cream; 400 mg cream applied to 16 cm 2; external application; once daily, for 12 weeks) also significantly improves scar appearance without reducing tissue strength in porcine injury models when applied topically [1]. Animal Model: Porcine excision injury model (female Juvenile pigs, 18-20 kg) [1] Dosage: 0.5, 1.5, or 3%, oil in water cream; 400 mg cream applied to 16 cm 2 Administration: External application; 1, 2 and 3 weeks post-injury; once dayly, for 12 weeks Result: Exhibited significantly higher scores for the 3% treated scars indicating significant improvement in scar appearance. |
分子量 | 265.25 |
分子式 | C10H10F3NO2S |
CAS No. | 2584947-54-4 |
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-6302 2584947-54-4 Inhibitor inhibitor inhibit