CP 640186 Usage And Synthesis
Uses
CP 640186 can be used to regulate porcine reproductive and respiratory syndrome virus infection via the AMPK-?ACC1 signaling pathway.
Definition
ChEBI: (3R)-1'-(9-anthrylcarbonyl)-3-(morpholin-4-ylcarbonyl)-1,4'-bipiperidine is a member of anthracenes, a member of morpholines, a member of bipiperidines and a N-acylpiperidine.
in vivo
CP-640186 (oral gavage; 4.6-21 mg/kg; once) demonstrates acute efficacy[1].
CP-640186 (intravenous injection and oral gavage; Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg; once) shows lowe drug exposure in the rat than the ob/ob mouse at equal doses[1].
CP-640186 (oral gavage; 100 mg/kg; once) treatment shows a complete shift from carbohydrate utilization to fatty acid utilization as a source of energy at high exposure level[1].
| Animal Model: | Male ob/ob mice[1] |
| Dosage: | 4.6-21 mg/kg |
| Administration: | Oral gavage; 4.6-21 mg/kg; once |
| Result: | Demonstrated acute efficacy for up to 8 h after oral administration, exhibiting ED50 values of 4.6, 9.7, and 21 mg/kg, at 1, 4, and 8 h, respectively, after treatment. |
| Animal Model: | Male Sprague-Dawley rats[1] |
| Dosage: | Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg |
| Administration: | Intravenous injection and oral gavage; Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg; once |
| Result: | Showed a plasma half-life of 1.5 h, a bioavailability of 39%, a Clp of 65 ml/min/kg, a Vdss of 5 liters/kg, an oral Tmax of 1.0 h, an oral Cmax of 345 ng/mL, and an oral AUC0-∞ of 960 ng?h/mL. |
| Animal Model: | Male ob/ob mice[1] |
| Dosage: | Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg |
| Administration: | Intravenous injection and oral gavage; Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg; once |
| Result: | Showed a plasma half-life of 1.1 h, a bioavailability of 50%, a Clp of 54 ml/min/kg, an oral Tmax of 0.25 h, an oral Cmax of 2177 ng/mL, and an oral AUC0-∞ of 3068 ng?h/mL. |
| Animal Model: | Twenty male Sprague-Dawley rats (350-400 g) fasted and then refed a high sucrose diet for 2 days; additional eight rats fasted for 24 h[1] |
| Dosage: | 100 mg/kg |
| Administration: | Oral gavage; 100 mg/kg; once |
| Result: | Resulted in time-dependent reductions in RQ (a ratio of CO2 production to O2 consumption) of up to 64%. |