产品
编 号:F495951
分子式:C19H20N4O
分子量:320.39
产品类型
结构图
CAS No: 882256-55-5
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产品详情
生物活性:
iGOT1-01 is a potent aspartate aminotransferase 1 (glutamate oxaloacetate transaminase 1; GOT1) inhibitor. iGOT1-01 has IC50s of 85 μM and 11.3 μM in MDH coupled GOT1 enzymatic assay and GOT1/GLOX/HRP assay, respectively. iGOT1-01 has anti-cancer activity.
体内研究:
iGOT1-01 (compound 1a; 20 mg/kg; oral) has reasonable bioavailability and exposure properties (t1/2=0.7 hours, Cmax=4133 ng/mL, AUC(0-24 hours)=11734 hour?ng/mL). Animal Model:Female CD1 mice with 9 weeks old
Dosage:20 mg/kg (Pharmacokinetic Analysis)
Administration:Oral
Result:Has reasonable bioavailability and exposure properties (t1/2=0.7 hours, Cmax=4133 ng/mL, AUC(0-24 hours)=11734 hour?ng/mL).
体外研究:
iGOT1-01 has an IC50 of 84.6 μM in the GOT1/MDH1 assay. No inhibitory activity is observed for iGOT1-01 against MDH1 alone at 100 μM. iGOT1-01 (3.125-200 μM; for 3 h) reveals little to no toxicity using two readouts of cell viability in PaTu8902 pancreatic and DLD1 colon cancer cells.