产品
编 号：F292638
分子式：C22H45N3O3
分子量：399.61
分子式：C22H45N3O3
分子量：399.61
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 250694-07-6
产品详情
生物活性：
Teglicar is a selective and reversible orally active liver isoform of carnitine palmitoyl-transferase 1 (L-CPT1) inhibitor with an IC50 value of 0.68 μM and a Ki value of 0.36 μM. Teglicar has a potential antihyperglycemic propert. Teglicar can be used for the research of diabetes and neurodegenerative disease including Huntington's disease (HD).
体内研究：
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.Animal Model:SD rats
Dosage:80 mg/kg, 5.3 mg/kg
Administration:oral, 80 mg/kg, once a day, for 30 days or infusion, 5.3 mg/kg/h, for 3 h
Result:Reduced basal insulin levels, showed a higher triglyceride and low glycogen content in the liver, without any change in liver weight.Showed a rapid drop in glycemia, suppressed EGP (EGP2) diminished by 62% and not affected peripheral glucose utilization (GU).
Animal Model:C57BL6/J mice
Dosage:50 mg/kg, 100 mg/kg
Administration:gavage, 50 mg/kg, single or long-term 100 mg/kg/day for 30 days.
Result:Did not modify etomoxir-induced M-CPT1 inhibition and failed to determine significant changes in 2-DG heart uptake, heart weights, and triglyceride content.
Animal Model:db/db mice
Dosage:50 mg/kg
Administration:gavage, 50 mg/kg, twice a day, for 45 days
Result:Induced a significant reduction of postabsorptive serum glucose, reduced serum fructosamine and average daily water consumption, increased Serum FFAs, but did not change insulin levels, triglycerides, alanine aminotransferase, also induced a significant reduction of glucose AUC during ITT.Did not induce any variation in the content of PPAR-α and its target gene product MCAD and peroxisomal b-oxidation in liver and heart of db/db mice.
Animal Model:High-fat diet C57BL/6J mice
Dosage:30 mg/kg
Administration:30 mg/kg, twice a day, for 26 days
Result:Did not affect food intake, did not change body weight and serum FFAs and triglycerides and did not affect glucose intolerant.
体外研究：
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.
Teglicar is a selective and reversible orally active liver isoform of carnitine palmitoyl-transferase 1 (L-CPT1) inhibitor with an IC50 value of 0.68 μM and a Ki value of 0.36 μM. Teglicar has a potential antihyperglycemic propert. Teglicar can be used for the research of diabetes and neurodegenerative disease including Huntington's disease (HD).
体内研究：
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.Animal Model:SD rats
Dosage:80 mg/kg, 5.3 mg/kg
Administration:oral, 80 mg/kg, once a day, for 30 days or infusion, 5.3 mg/kg/h, for 3 h
Result:Reduced basal insulin levels, showed a higher triglyceride and low glycogen content in the liver, without any change in liver weight.Showed a rapid drop in glycemia, suppressed EGP (EGP2) diminished by 62% and not affected peripheral glucose utilization (GU).
Animal Model:C57BL6/J mice
Dosage:50 mg/kg, 100 mg/kg
Administration:gavage, 50 mg/kg, single or long-term 100 mg/kg/day for 30 days.
Result:Did not modify etomoxir-induced M-CPT1 inhibition and failed to determine significant changes in 2-DG heart uptake, heart weights, and triglyceride content.
Animal Model:db/db mice
Dosage:50 mg/kg
Administration:gavage, 50 mg/kg, twice a day, for 45 days
Result:Induced a significant reduction of postabsorptive serum glucose, reduced serum fructosamine and average daily water consumption, increased Serum FFAs, but did not change insulin levels, triglycerides, alanine aminotransferase, also induced a significant reduction of glucose AUC during ITT.Did not induce any variation in the content of PPAR-α and its target gene product MCAD and peroxisomal b-oxidation in liver and heart of db/db mice.
Animal Model:High-fat diet C57BL/6J mice
Dosage:30 mg/kg
Administration:30 mg/kg, twice a day, for 26 days
Result:Did not affect food intake, did not change body weight and serum FFAs and triglycerides and did not affect glucose intolerant.
体外研究：
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.
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