DDR-TRK-1,1934246-19-1

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DDR-TRK-1

CAS No. : 1934246-19-1

MCE 国际站：DDR-TRK-1

产品活性：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。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Discoidin Domain Receptor

In Vitro: DDR-TRK-1 is a promising candidate, with an IC₅₀ value of 9.4 nM against DDR1. DDR-TRK-1 also exhibits reasonable pharmacokinetic (PK) properties, with an oral bioavailability of 66.8% and a T_1/2 value 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 (K_d) value of 4.7 nM.

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.

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