Powder: -20°C for 3 years | In solvent: -80°C for 1 year
XL-784 is a selective inhibitor of matrix metalloproteinases (MMP)(IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1,MMP-2,MMP-3,MMP-8,MMP-9,MMP-13,respectively).
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 1,710 | 5日内发货 | ||
5 mg | ¥ 2,890 | 5日内发货 | ||
25 mg | ¥ 10,500 | 8-10周 | ||
50 mg | ¥ 13,700 | 8-10周 | ||
100 mg | ¥ 20,800 | 8-10周 |
产品描述 | XL-784 is a selective inhibitor of matrix metalloproteinases (MMP)(IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1,MMP-2,MMP-3,MMP-8,MMP-9,MMP-13,respectively). |
靶点活性 | MMP1:1900 nM, MMP2:0.81 nM, MMP9:18 nM, MMP8:10.8 nM, MMP13:0.56 nM, MMP3:120 nM |
体外活性 | XL-784 is a low-molecular-weight (1,122 g/mol) MMPs inhibitor. XL-784 potently inhibits MMP-2, MMP-13, and ADAM10 [TNF-α-converting enzyme (TACE)] activity in vitro(IC50 values in the range of 1-2 nM). XL-784 also inhibits MMP-9 (IC50 ~20 nM) activity and ADAM17 (IC50 ~70 nM) also known as TACE. However, XL-784 exhibits low potency for inhibition of MMP-1 (IC50 ~2,000 nM)[1]. |
体内活性 | Treatment with all doses of XL-784 and doxycycline are effective in inhibiting aortic dilatation. There is a clear dose-response relationship between XL-784 and reductions in aortic dilatation at harvest (50 mg/kg 140.4% ±3.2%; 125 mg/kg 129.3% ±5.1%; 250 mg/kg 119.2%±3.5%; all Ps<0.01 compared to control). This continues with the higher doses (375 mg/kg 88.6%±4.4%; 500 mg/kg 76.0%±3.5%). he two doses of the highest dose of XL-784 tested were more effective than doxycycline in inhibiting the maximum expansion of the aorta after elastase infusion (112.2%±2.0%, P<0.05) [2]. |
分子量 | 1126.17 |
分子式 | C42H46Cl2F4MgN6O16S2 |
CAS No. | 1224964-36-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 110 mg/mL (200.03 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 0.888 mL | 4.4398 mL | 8.8797 mL | 22.1991 mL |
5 mM | 0.1776 mL | 0.888 mL | 1.7759 mL | 4.4398 mL | |
10 mM | 0.0888 mL | 0.444 mL | 0.888 mL | 2.2199 mL | |
20 mM | 0.0444 mL | 0.222 mL | 0.444 mL | 1.11 mL | |
50 mM | 0.0178 mL | 0.0888 mL | 0.1776 mL | 0.444 mL | |
100 mM | 0.0089 mL | 0.0444 mL | 0.0888 mL | 0.222 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。
XL-784 1224964-36-6 Proteases/Proteasome MMP XL 784 XL784 Inhibitor inhibitor inhibit