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产品价格:电议      采购度:1639      原产地:美洲
发布时间:2021/9/13 20:06:31 所属地区:国外 国外
简要描述:
ML351 是一种有效且高度特异的 15-LOX-1 抑制剂,其 IC50 of 200 nM。ML351 对相关同工酶 (5-LOX、血小板 12-LOX、15-LOX-2、绵羊 COX-1 和人COX-2) 表现出良好的选择性(>250倍)。ML351 对 T1D 非肥胖糖尿病小鼠模型的血糖异常和β细胞氧化应激有抑制作用。
标签:ml351
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CAS No. : 847163-28-4
MCE 站:ML351
产品活性:ML351 是一种有效且高度特异的 15-LOX-1 抑制剂,其 IC50 of 200 nM。ML351 对相关同工酶 (5-LOX、血小板 12-LOX、15-LOX-2、绵羊 COX-1 和人COX-2) 表现出良好的选择性(>250倍)。ML351 对 T1D 非肥胖糖尿病小鼠模型的血糖异常和β细胞氧化应激有抑制作用。
研究领域:Metabolic Enzyme/Protease
作用靶点:Lipoxygenase
In Vitro: ML351 (1-50 μM; 24 hours) displays no deleterious effects on cellular apoptosis (by caspase activity assay).
ML351 (10-50 μM; 24 h) protects mouse islets in a T1D model in vitro. Islets exposed to proinflammatory cytokines exhibits increased insulin release at 2.5 mM glucose and impaired insulin release in response to 25 mM glucose. However, ML351 restores insulin secretion at 2.5 mmol/L glucose to control levels, and insulin release in response to 25 mM glucose is significantly improved compared with treatment with proinflammatory cytokines alone.
ML351 reverses the stimulation of ROS production in mouse islets in response to proinflammatory cytokines in vitro.
In Vivo: ML351 (0-48 mg/kg; before the beginning of the STZ series and concluding 5 days after the last dose of STZ) protects against diabetes development in an STZ β-cell injury model. ML351 at 24 mg/kg (M24)+ STZ shows significantly less weight reduction compares with control group. M24 shows almost complete protection from hyperglycemia. But M48 and M0 exhibits frank hyperglycemia by day 9 of the study and significantly impaired GTTs.
ML351 (intraperitoneal injection; 0-24 mg/kg; daily for 2 weeks) leads to improved glycemic control and significantly reduced insulitis. The reduction of β-cell death in NOD mice has been suggested to lead to reductions in insulitis, likely by mitigating the chemotactic signals released by dying β-cells. NOD + M24 animals exhibited improved glycemic control compared with NOD + M0 animals.
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更新时间:2024/1/2 10:18:09
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