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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
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.
In Vitro
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Col4a3 –/– mice, a mouse model phenocopying Alport syndrome . 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.
Form:Solid