DDR1-IN-4 (Compound 2.45) is a selective and potent Discoidin Domain Receptor 1 (DDR1) autophosphorylation inhibitor, with IC 50 values of 29 nM and 1.9 μM for DDR1 and DDR2, respectively.

DDR1-IN-4 (Compound 2.45) shows a clear dose-dependent inhibition of DDR1 phosphorylation in HT1080 cells overexpressing DDR1, with greater than 70% inhibition of phosphorylation at a concentration of 1 μM, and retaining selectivity over inhibition of DDR2[1].

DDR1-IN-4 (Compound 2.45, ip, 90 mg/kg) preserves renal function and reduces tissue damage in Col4a3 –/– mice (the preclinical mouse model of Alport syndrome) when employing a therapeutic dosing regime, indicating the real therapeutic value of selectively inhibiting DDR1 phosphorylation in vivo[1]. Animal Model: Col4a3 –/– mice, a mouse model phenocopying Alport syndrome[1]. Dosage: 90 mg/kg. Administration: Injected intraperitoneally daily. Result: Resulted in a significant reduction of fibrosis evaluated by Picro Sirius Red, smooth muscle actin staining, and collagen I accumulation. Significantly reduces the levels of pDDR1 in Col4a3 knockout mice compared to controls.

2125676-13-1

C23H20BrF3N6O3

565.34

DDR1-IN-4;DDR1-IN-4

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years