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

IC50: 9.4 nM (DDR1)^[1].

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 T_1/2value 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 (K_d) value of 4.7 nM^[1].

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].

492.50

C₂₆H₂₃F₃N₆O

1934246-19-1

Room temperature in continental US; may vary elsewhere.

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