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编 号:F239200
分子式:C29H32N4O6S
分子量:564.65
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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生物活性:
Ruboxistaurin (LY333531) mesylate is an orally active, selective and ATP competitive PKCβ inhibitor with IC50 values of 4.7 and 5.9 nM for PKCβI and PKCβII, respectively. Ruboxistaurin mesylate can be used for the research of eye disorders, heart failure and diabetes.

体内研究:
Ruboxistaurin mesylate (0.1, 1.0 和 10.0 mg/kg;口服,每日 1 次,共 3 周) 抑制糖尿病早期视网膜微循环中白细胞滞留的增加。Animal Model:Male long-evans rats with streptozotocin induced diabetes
Dosage:0.1, 1.0 and 10.0 mg/kg
Administration:Oral administration; 0.1, 1.0 and 10.0 mg/kg, once daily for 4 weeks
Result:Significantly decreased the number of leukocytes in the retinal microcirculation of rats with streptozotocin induced diabetes.

体外研究:
Ruboxistaurin mesylate 对 PKCα,PKCβI,PKCβII,PKCγ,PKCδ,PKCε 和 PKCη 的 IC50 值分别为 0.36,0.0047,0.0059,0.30,0.25,0.60 和 0.052 μM。Ruboxistaurin mesylate 抑制 Ca calmodulin 和大鼠脑 PKC 的 IC50 分别为 6.2 和 0.32 μM。Ruboxistaurin mesylate (10 和 400 nM;4 天) 显著抑制正常血糖 (NG) 条件下葡萄糖诱导的单核细胞粘附。
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