Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DDR-TRK-1 是 DDR1的一个选择性抑制剂,其 IC50 值为 9.4 nM。DDR-TRK-1 也抑制 TRK 激酶家族。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,290 | 现货 | ||
2 mg | ¥ 1,930 | 现货 | ||
5 mg | ¥ 2,990 | 现货 | ||
10 mg | ¥ 4,390 | 现货 | ||
25 mg | ¥ 6,910 | 现货 | ||
50 mg | ¥ 9,480 | 现货 | ||
100 mg | ¥ 12,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,460 | 现货 |
产品描述 | DDR-TRK-1 is a selective discoid domain receptor 1 (DDR1) inhibitor with IC50 value of 9.4 nM. DDR-TRK-1 also inhibits the TRK family. |
靶点活性 | DDR1:9.4 nM |
体外活性 | DDR-TRK-1 is a promising candidate with an IC50 value of 9.4 nM relative to DDR1. DDR-TRK-1 also exhibited reasonable pharmacokinetic (PK) properties. At an oral dose of 20 mg/kg in rats, the oral bioavailability was 66.8%, and the T1/2 value was 1.25 h. However, the area under the concentration-time curve (AUC) value of DDR-TRK-1 in mice was significantly higher than that in rats, indicating that its absorption performance in mice was good. By determining the binding affinity of DDR1-IN-3 and DDR1 protein, the inhibitory effect of DDR1 on DDR1-IN-3 can be further verified. The results show that DDR-TRK-1 is closely bound to DDR1, and the binding constant (Kd) value is 4.7 nM[1]. |
体内活性 | DDR-TRK-1 can prevent blm-induced pathological changes in a dose-dependent manner. These results agree with the expression levels of fibrosis markers in the lung tissue, including lysates, including fibronectin and α-smooth muscle actin (SMA). Further analysis also showed that the use of DDR-TRK-1 resulted in a dose-dependent inhibition of hydroxyproline content, a unique amino acid found in collagen. The above data indicate that DDR-TRK-1 has good therapeutic potential for blm-induced pulmonary fibrosis[1]. |
分子量 | 492.5 |
分子式 | C26H23F3N6O |
CAS No. | 1934246-19-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (101.52 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0305 mL | 10.1523 mL | 20.3046 mL | 50.7614 mL |
5 mM | 0.4061 mL | 2.0305 mL | 4.0609 mL | 10.1523 mL | |
10 mM | 0.203 mL | 1.0152 mL | 2.0305 mL | 5.0761 mL | |
20 mM | 0.1015 mL | 0.5076 mL | 1.0152 mL | 2.5381 mL | |
50 mM | 0.0406 mL | 0.203 mL | 0.4061 mL | 1.0152 mL | |
100 mM | 0.0203 mL | 0.1015 mL | 0.203 mL | 0.5076 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。
DDR-TRK-1 1934246-19-1 Tyrosine Kinase/Adaptors Discoidin Domain Receptor (DDR) DDRTRK1 DDR TRK 1 Inhibitor inhibitor inhibit