Database
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| 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 | ||||||