F02060101 | Mitochondrial fatty acid beta oxidation

Compound Dose Time Species Model Method Action Result Positive criterion Reference
Tamoxifen affect Positive 227
Perhexiline 100 μM 5 minutes preincubation; 10 minutes mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of beta oxidation decrease Positive p < 0.01 193
Perhexiline 100 μM 5 minutes preincubation; 10 minutes mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of beta oxidation decrease Positive p < 0.01 193
Perhexiline 200 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline 400 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline 800 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline 1200 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline 200 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline 400 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline 800 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline 1200 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline 1600 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline 400 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.05 193
Perhexiline 800 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline 1200 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline 1600 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline decrease Positive 16
Perhexiline decrease Positive 16
buprenorphine 100 μM rat liver mitochondria the mitochondrial membrane potential assessed by the fluorescence of safranine. affect Positive 235
Tianeptine 0.0625 mmol/kg i.p. mouse in vivo affect Positive 237
Perhexiline decrease Positive 17
Perhexiline decrease Positive 17
Trimetazidine decrease Positive 17
ranolazine decrease Positive 17
tetracyclines mouse liver mitochondria affect Positive 236
5-Hydroxydecanoate 100 μm decrease Positive 189
5-Hydroxydecanoate K1/2 values 45-75 microM heart and liver mitochondria from rat decrease Positive 190
Ibuprofen affect Positive 239
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, affect 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, affect 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, affect Positive IC50 240
FOX-988 decrease Positive 28
Acetaminophen >400μM >400 mice Lean mice vs Ob/ob mice Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform Positive EC20 227
Sdz-51641 decrease Positive 28
Salicylic acid decrease Positive 32
Irinotecan 6μM 10 mice Lean mice vs Ob/ob mice Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform Positive EC20 227
Methotrexate 44μM 42 mice Lean mice vs Ob/ob mice Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform Positive EC20 227
Troglitazone affect Positive 227
Valproic Acid affect Positive 227
Perhexiline decrease Positive 35
Amiodarone 20 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
Amiodarone 50 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
Amiodarone 80 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
Amiodarone 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
benzarone 20 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
benzarone 50 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
benzarone 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
benzbromarone 2 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.05 4
benzbromarone 5 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
benzbromarone 10 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
benzbromarone 50 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
2‐Butylbenzofuran 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
Etomoxir decrease Positive 35
Salicylic acid decrease Positive 35
Carbamazepine >400μM 341 mice Lean mice vs Ob/ob mice Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform Positive EC20 227
Diclofenac 47μM 11* mice Lean mice vs Ob/ob mice Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform Positive EC20 227
Ibuprofen 287μM 80* mice Lean mice vs Ob/ob mice Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform Positive EC20 227
Amiodarone 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of acyl‐CoA dehydrogenase activity decrease Positive 28% inhibition 4
benzarone 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of acyl‐CoA dehydrogenase activity decrease Positive 33% inhibition 4
benzbromarone 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of acyl‐CoA dehydrogenase activity decrease Positive 34% inhibition 4
2‐Butylbenzofuran 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of acyl‐CoA dehydrogenase activity decrease Positive 22% inhibition 4
benzarone 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of β‐ketothiolase activity decrease Positive 11% inhibition 4
benzbromarone 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of β‐ketothiolase activity decrease Positive 25% inhibition 4
Salicylic acid >400μM >400 mice Lean mice vs Ob/ob mice Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform Positive EC20 227
Tamoxifen 4μM 11 mice Lean mice vs Ob/ob mice Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform Positive EC20 227
Perhexiline rat hepatocytes affect Positive 238
Zidovudine 79μM 83 mice Lean mice vs Ob/ob mice Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform Positive EC20 227
Acetaminophen affect Positive 227
amineptine decrease Positive 54
pirprofen decrease Positive 59
Salicylic acid affect Positive 227
Ibuprofen affect Positive 227
TDGA <0.05/0.04 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
POCA 10.4/95.9 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
Etomoxir 0.29/0.34 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
DET 1.8/4.4 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
aminocarnitine −/− human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
Carnitine 0.5mM 24hr U-937, MCF-7, and T47D quantifies the conversion of [9,10-3H(N)]-palmitic acid to 3H2O with diffusion stimulate Positive 273
AICAR 1mM 24hr U-937, MCF-7, and T47D quantifies the conversion of [9,10-3H(N)]-palmitic acid to 3H2O with diffusion stimulate Positive 273
AICAR stimulate Positive 273
palmitoylaminocarnitine 2.8/0.27 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
ST1326 4.0/0.98 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
ST2425 0.73/0.03 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
Trimetazidine 20.5/>100 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
Perhexiline 22.4/21.4 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
Amiodarone 28.5/>100 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
Oxfenicine >100/>100 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
oxfenicine metabolite 33.3/>100 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
RO-25-0187 25.5/>100 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
Hypoglycin A Positive 232
4-Pentenoic acid Positive 232
2-bromooctanoic acid Positive 232
2-tetradecylglycidic acid Positive 232
2-bromopalmitic acid Positive 232
Palmitoylcarnitine Positive 232
Perhexiline 5 μM 72 hours rat; Sprague-Dawley Crl:CD-1 (ICR) BR hepatocytes Measurement of beta oxidation decrease Positive p < 0.05 193
Perhexiline 25 μM 24 hours rat; Sprague-Dawley Crl:CD-1 (ICR) BR hepatocytes Measurement of beta oxidation decrease Positive p < 0.05 193
Amiodarone affect Positive 227
Tamoxifen affect Positive 227