目錄:MedChemExpress LLC>>生化試劑>> VU6015929 | MCE
CAS | 2442597-56-8 | 純度 | 98.03% |
---|---|---|---|
分子量 | 485.43 | 分子式 | C??H??F?N?O? |
供貨周期 | 現貨 | 規格 | 5 mg |
貨號 | HY-135401 | 應用領域 | 醫療衛生,化工,生物產業,制藥 |
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CAS No. : 2442597-56-8
產品活性:VU6015929 is a potent, selective and orally active dual discoidin domain receptor 1/2 (DDR1/2) inhibitor with IC50s of 4.67 nM and 7.39 nM, respectively. VU6015929 potently blocks collagen-induced DDR1 activation and collagen-IV production.
研究領域:Protein Tyrosine Kinase/RTK
作用靶點:Discoidin Domain Receptor
In Vitro: VU6015929 (Compound 7e; 4-100 nM; 24 hours; HEK293-DDR1b cells) treatment inhibits collagen I-induced DDR1 phosphorylation in a dose dependent manner. Analysis of the phosphorylated DDR1/total DDR1 ratio reveals an IC50 for VU6015929 of 0.7078 nM.
In Vivo: VU6015929 (Compound 7e) is further evaluated in a rat IV (0.5 mg/kg)/PO (3 mg/kg) PK study in a 10% EtOH/40% PEG400/50% saline vehicle. VU6015929 displays a good in vitro:in vivo correlation (IVIC), with moderate in vivo clearance (CLp = 34.2 mL/min/kg), an ~3 hour half-life, moderate volume of distribution at steady state (Vss = 4.3 L/kg) and 12.5% oral bioavailability with a rapid Tmax (0.75 hr).
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