Teglicar

Research use only, not for human use.

Teglicar (ST-1326) is a potent, selective and reversible inhibitor of liver carnitine palmitoyl-transferase 1 (L-CPT1) with IC50 of 0.68 uM, Ki of 0.36 uM.

Teglicar (ST-1326) is a potent, selective and reversible inhibitor of liver carnitine palmitoyl-transferase 1 (L-CPT1) with IC50 of 0.68 uM, Ki of 0.36 uM; displays an extraordinarily high selectivity (39-fold) toward the liver isoform over the heart isoform (muscle-CPT1;M-CPT1); reduces gluconeogenesis and improves glucose homeostasis, shows antiketotic and antidiabetic activity in diabetic db/db mice; also inhibits fatty acid oxidation associated with cell growth arrest, mitochondrial damage, and apoptosis induction in leukemia cell lines; orally active.Diabetes Phase 2 Discontinued.

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 (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.

ST-1326 | ST1326

Others

Other Targets

Other Targets

Metabolic Disease

Diabetes

250694-07-6

399.62

C22H45N3O3

>98% (HPLC)

In Vitro:?Ethanol : 100 mg/mL (250.24 m)

CCCCCCCCCCCCCCNC(=O)NC(CC(=O)[O-])C[N+](C)(C)C

(R)-4-Trimethylammonio-3-[(tetradecylcarbamoyl)amino]butyrate

(-20℃)

With Ice Pack

≥ 2 years