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.
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