T021 Source: Uniprot

enzymecarnitine palmitoyltransferases I (CPT-I)
Transferase Acyltransferase
Full Name carnitine palmitoyltransferases I
Subcellular Location Cell junction, synapse Cell projection, axon Cell projection, dendrite Endoplasmic reticulum Mitochondrion outer membrane Multi-pass membrane protein
EC numbers 2.3.1.21

Compound Dose Time Species Model Method Result Positive criterion Reference
Etomoxir Positive 35
Perhexiline Positive 16
Perhexiline Positive 17
aminocarnitine 76.4/27.3 human/rat recombinant Pichia pastoris Membrane Preparations spectrophotometric assay with DTNB Positive IC50 (μM) 333
palmitoylaminocarnitine 2.67/− human/rat recombinant Pichia pastoris Membrane Preparations spectrophotometric assay with DTNB Positive IC50 (μM) 333
ST1326 1.05/1.45 human/rat recombinant Pichia pastoris Membrane Preparations spectrophotometric assay with DTNB Positive IC50 (μM) 333
ST2425 1.70/− human/rat recombinant Pichia pastoris Membrane Preparations spectrophotometric assay with DTNB Positive IC50 (μM) 333
Trimetazidine >100/− human/rat recombinant Pichia pastoris Membrane Preparations spectrophotometric assay with DTNB Negative IC50 (μM) 333
Perhexiline >100/− human/rat recombinant Pichia pastoris Membrane Preparations spectrophotometric assay with DTNB Negative IC50 (μM) 333
Amiodarone >100/− human/rat recombinant Pichia pastoris Membrane Preparations spectrophotometric assay with DTNB Negative IC50 (μM) 333
Oxfenicine >100/− human/rat recombinant Pichia pastoris Membrane Preparations spectrophotometric assay with DTNB Negative IC50 (μM) 333
oxfenicine metabolite >100/− human/rat recombinant Pichia pastoris Membrane Preparations spectrophotometric assay with DTNB Negative IC50 (μM) 333
RO-25-0187 2.4/− human/rat recombinant Pichia pastoris Membrane Preparations spectrophotometric assay with DTNB Positive IC50 (μM) 333
aminocarnitine >100 human/rat recombinant Pichia pastoris Membrane Preparations spectrophotometric assay with DTNB Negative IC50 (μM) 333
palmitoylaminocarnitine 21.7 human/rat recombinant Pichia pastoris Membrane Preparations spectrophotometric assay with DTNB Positive IC50 (μM) 333
ST1326 5.4 human/rat recombinant Pichia pastoris Membrane Preparations spectrophotometric assay with DTNB Positive IC50 (μM) 333
ST2425 85.3 human/rat recombinant Pichia pastoris Membrane Preparations spectrophotometric assay with DTNB Positive IC50 (μM) 333
Trimetazidine >100 human/rat recombinant Pichia pastoris Membrane Preparations spectrophotometric assay with DTNB Negative IC50 (μM) 333
Perhexiline >100 human/rat recombinant Pichia pastoris Membrane Preparations spectrophotometric assay with DTNB Negative IC50 (μM) 333
Amiodarone >100 human/rat recombinant Pichia pastoris Membrane Preparations spectrophotometric assay with DTNB Negative IC50 (μM) 333
Oxfenicine >100 human/rat recombinant Pichia pastoris Membrane Preparations spectrophotometric assay with DTNB Negative IC50 (μM) 333
oxfenicine metabolite 60.3 human/rat recombinant Pichia pastoris Membrane Preparations spectrophotometric assay with DTNB Positive IC50 (μM) 333
RO-25-0187 0.16 human/rat recombinant Pichia pastoris Membrane Preparations spectrophotometric assay with DTNB Positive IC50 (μM) 333
Valproic Acid Positive 227
Amiodarone Positive 227
Perhexiline Positive 35
Tamoxifen Positive 227
Tamoxifen Positive 227
Etomoxir 5 μM T cell Positive 257
Perhexiline 77 μmol/L rat cardiac mitochondria CPT-1 activity was measured by the formation of palmitoyl-[3H]-carnitine from palmitoyl-CoA and [3H]-I- carnitine, Positive IC50 240
Perhexiline 148 μmol/L rat hepatic mitochondria CPT-1 activity was measured by the formation of palmitoyl-[3H]-carnitine from palmitoyl-CoA and [3H]-I- carnitine, Positive IC50 240
Amiodarone 228 μmol/L rat cardiac and hepatic mitochondria CPT-1 activity was measured by the formation of palmitoyl-[3H]-carnitine from palmitoyl-CoA and [3H]-I- carnitine, Positive IC50 240