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CAS No. : 250694-07-6
MCE 国际站:Teglicar
产品活性:Teglicar 是一种选择性、可逆性的肉碱棕榈酰转移酶1 (L-CPT1) 肝脏亚型抑制剂,具有口服活性,其 IC50 值为 0.68 μM, Ki 值为 0.36 μM。Teglicar 具有潜在的抗高血糖特性。Teglicar 可用于糖尿病和神经退行性疾病的研究,包括亨廷顿病(HD)。
研究领域:Metabolic Enzyme/Protease
作用靶点:Endogenous Metabolite
In Vitro: Teglicar has L-CPT1 inhibitory activity with an IC50 value of 0.68 μM and a Ki value of 0.36 μM.
Teglicar (10 μM; 2 h) induces a concentration-dependent reduction of ketone bodies and glucose production.
In Vivo: Teglicar (oral, 80 mg/kg, once a day, for 30 days or infusion, 5.3 mg/kg/h, for 3 h) reduces the endogenous glucose production (262%) without affecting peripheral glucose utilization in SD rats.
Teglicar (gavage, 50 mg/kg, single or long-term 100 mg/kg/day for 30 days) not affects heart 2-[3H]deoxyglucose uptake in C57BL6/J mice.
Teglicar (gavage, 50 mg/kg, twice a day, for 45 days) reduces postabsorptive glycemia (238%), water consumption (231%), and fructosamine (230%) in db/db mice.
Teglicar (30 mg/kg, twice a day, for 26 days) normalized glycemia (219%) and insulinemia (253%) and increases HTGC but not affects liver and peripheral insulin sensitivity in high-fat diet C57BL/6J mice.
Teglicar (oral, 50 μM, was added to the surface of fly food, 1, 8, 12, and 15 days) ameliorates the neurodegenerative phenotype in a drosophila Huntington's Disease Model by acting on the expression of carnitine-related genes.
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