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DDR-TRK-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
DDR-TRK-1图片
CAS NO:1934246-19-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
DDR-TRK-1 是圆盘状受体 1 (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。
生物活性

DDR-TRK-1 is a selectiveDiscoidin Domain Receptor1(DDR1)inhibitor, with anIC50value of 9.4 nM. DDR-TRK-1 also inhibitsTRKfamily.

IC50& Target

IC50: 9.4 nM (DDR1)[1].

体外研究
(In Vitro)

DDR-TRK-1 is a promising candidate, with an IC50value of 9.4 nM against DDR1. DDR-TRK-1 also exhibits reasonable pharmacokinetic (PK) properties, with an oral bioavailability of 66.8% and a T1/2value of 1.25 h at an oral dose of 20 mg/kg in rats. However, the area under concentration–time curve (AUC) value of DDR-TRK-1 in mice is obviously higher than that in rats, suggesting its good absorption property in mice. The DDR1 inhibition of DDR1-IN-3 is further validated by determining its binding affinity with the DDR1 protein. It is shown that DDR-TRK-1 bounds tightly to DDR1, with a binding constant (Kd) value of 4.7 nM[1].

体内研究
(In Vivo)

DDR-TRK-1 prevents these BLM-induced pathological changes in a dose-dependent manner. These results agree with the expression levels of fibrotic markers in lung tissue lysates, including fibronectin and α-smooth muscle actin (SMA). Further analyses also reveal that the administration of DDR-TRK-1 cause a dose-dependent suppression in the content of hydroxyproline, a unique amino acid found in collagen. The above data collectively indicate the promising therapeutic potential of DDR-TRK-1 against the BLM-induced pulmonary fibrosis[1].

分子量

492.50

Formula

C26H23F3N6O

CAS 号

1934246-19-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.