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编 号：F756954
分子式：C19H16F3N3O3
分子量：391.34
分子式：C19H16F3N3O3
分子量：391.34
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CAS No: 2925249-49-4
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生物活性：
MMP-13-IN-1 is a potent and selective inhibitor of MMP-13 with a IC50 value of 16 nM. MMP-13-in-1 can be used for atherosclerosis research.
体内研究：
MMP-13-IN-1 (compound 5j) (2.5 mg/kg; 使用放射性示踪剂前 15 分钟静脉注射) 在 ApoE?/? 小鼠模型中表现出代谢器官摄取低，心肌放射性保留最少，肾脏清除率高，代谢稳定性高的特点。MMP-13-IN-1 (compound 5j) (2.5 mg/kg; 使用放射性示踪剂前 15 分钟静脉注射) 显示最高的总体摄取和 ORO 阳性区域的最大共定位。Animal Model:ApoE?/? mice models
Dosage:2.5 mg/kg
Administration:Intravenous injection (i.v.); intravenously administered 15 min prior to the radiotracer
Result:Blood radioactivity continued to decrease between 30 and 60 min and stabilized thereafter.Displayed a significant reduction in liver uptake. Relatively low levels of radioactivity were observed in all other measured organs except for the pancreas and spleen.Resulted in a 23% decrease in aortic plaque uptake , indicating an extent of saturable binding.
MMP-13-IN-1 is a potent and selective inhibitor of MMP-13 with a IC50 value of 16 nM. MMP-13-in-1 can be used for atherosclerosis research.
体内研究：
MMP-13-IN-1 (compound 5j) (2.5 mg/kg; 使用放射性示踪剂前 15 分钟静脉注射) 在 ApoE?/? 小鼠模型中表现出代谢器官摄取低，心肌放射性保留最少，肾脏清除率高，代谢稳定性高的特点。MMP-13-IN-1 (compound 5j) (2.5 mg/kg; 使用放射性示踪剂前 15 分钟静脉注射) 显示最高的总体摄取和 ORO 阳性区域的最大共定位。Animal Model:ApoE?/? mice models
Dosage:2.5 mg/kg
Administration:Intravenous injection (i.v.); intravenously administered 15 min prior to the radiotracer
Result:Blood radioactivity continued to decrease between 30 and 60 min and stabilized thereafter.Displayed a significant reduction in liver uptake. Relatively low levels of radioactivity were observed in all other measured organs except for the pancreas and spleen.Resulted in a 23% decrease in aortic plaque uptake , indicating an extent of saturable binding.
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