Powder: -20°C for 3 years | In solvent: -80°C for 1 year
safironil 是一种新型抗纤维化化合物,是胶原蛋白合成的竞争性抑制剂。safironil 在体外实验中对由胶原蛋白I mRNA 或平滑肌α-actin 水平监测的成纤维细胞的激活,以及由I 型和III 型胶原蛋白和层粘连蛋白生产判断的纤维生成有抑制作用。safironil 在不改变总羟脯氨酸的情况下对肝脏肉芽肿的大小没有影响,但通过增加III 型和减少I 型胶原的沉积改变了纤维化的模式。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 680 | 现货 | ||
5 mg | ¥ 1,600 | 现货 | ||
10 mg | ¥ 2,390 | 现货 | ||
25 mg | ¥ 3,960 | 现货 | ||
50 mg | ¥ 5,760 | 现货 | ||
100 mg | ¥ 7,860 | 现货 | ||
500 mg | ¥ 15,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,490 | 现货 |
产品描述 | safironil is a novel antifibrotic compound and a competitive inhibitor of collagen synthesis. safironil inhibited in vitro experiments on fibroblast activation monitored by collagen I mRNA or smooth muscle alpha-actin levels, and fibrogenesis as judged by type I and type III collagen and laminin production. safironil had no effect on the size of liver granulomas without altering total hydroxyproline, but altered the pattern of fibrosis by increasing type III and decreasing type I collagen deposition. |
体外活性 | HOE 77, Safironil, and S 4682 are inhibitors of prolyl 4-hydroxylase, which is essential for thecollagen formation. Although HOE 77, Safironil, and S 4682 seem to work by inhibiting HSC activation, further studies will be required before their clinical application. alpha-Tocopherol, retinyl palmitate, and silybinin reduce lipid peroxidation and attenuate HSC activation in experimental models.[2] |
体内活性 | The present studies evaluate the mechanism of action of two novel antifibrotic compounds, HOE 077 and Safironil, which were designed as competitive inhibitors of collagen protein synthesis. Stellate cell activation, rather than collagen synthesis, proved to be the target of both HOE 077 and Safironil in the intact liver. In culture, the drugs not only prevented the activation of stellate cells but also accelerated their deactivation. They were no more effective in co-cultures containing hepatocytes than in pure stellate cell cultures, indicating that metabolic conversion of HOE 077 was not required. Interestingly, the response of cells from females was greater than that of male cells, leading to the conclusion that stellate activation is sexually dimorphic. This finding may be relevant to the observation that fibrosis in chronic viral hepatitis progresses less rapidly and that hepatocellular carcinoma is less frequent in females than in males.[1] |
分子量 | 309.36 |
分子式 | C15H23N3O4 |
CAS No. | 134377-69-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 30 mg/mL (96.97 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.2325 mL | 16.1624 mL | 32.3248 mL | 80.812 mL |
5 mM | 0.6465 mL | 3.2325 mL | 6.465 mL | 16.1624 mL | |
10 mM | 0.3232 mL | 1.6162 mL | 3.2325 mL | 8.0812 mL | |
20 mM | 0.1616 mL | 0.8081 mL | 1.6162 mL | 4.0406 mL | |
50 mM | 0.0646 mL | 0.3232 mL | 0.6465 mL | 1.6162 mL |
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。
Safironil 134377-69-8 Others Inhibitor inhibitor inhibit