说明： CP 640186是ACC (Acetyl-CoA carboxylase)抑制剂，对大鼠肝脏ACC1和骨骼肌ACC2的IC50分别为53 nM和61 nM。 Information CP 640186 CP 640186 is an isozyme-nonselective ACC (Acetyl-CoA carboxylase) inhibitor with IC50 values of 53 and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2, respectively. Targets ACC 55 nM In vitro CP-610431 inhibited ACC1 and ACC2 with IC50s of ∼50 nm. Inhibition was reversible, uncompetitive with respect to ATP, and non-competitive with respect to bicarbonate, acetyl-CoA, and citrate. CP-610431 also inhibited fatty acid synthesis, triglyceride (TG) synthesis, TG secretion, and apolipoprotein B secretion in HepG2 cells (ACC1) with EC50s of 1.6, 1.8, 3.0, and 5.7 μM, without affecting either cholesterol synthesis or apolipoprotein CIII secretion. It also inhibited both isozymes with IC50s of ∼55 nM in inhibiting HepG2 cell fatty acid and TG synthesis. CP-610431 stimulated fatty acid oxidation in C2C12 cells (ACC2) and in rat epitrochlearis muscle strips with EC50s of 57 nM and 1.3 μM. In vivo In rats, CP-640186 lowered hepatic, soleus muscle, quadriceps muscle, and cardiac muscle malonyl-CoA with ED50s of 55, 6, 15, and 8 mg/kg. Consequently, CP-640186 inhibited fatty acid synthesis in rats, CD1 mice, and ob/ob mice with ED50s of 13, 11, and 4 mg/kg, and stimulated rat whole body fatty acid oxidation with an ED50 of ∼30 mg/kg. Pharmacokinetic evaluation of CP-640186 in male Sprague-Dawley rats (intravenous dose, 5 mg/kg; oral dose, 10 mg/kg) yielded 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. At the same dose level, pharmacokinetic evaluation of CP-640186 in ob/ob mice yielded 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.
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CP 640186
Dangerous GoodsCAS number：591778-68-6 molecular formula：C30H35N3O3
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | 591778-68-6 | CP-640186 | CP 640186 | (R)-anthracen-9-yl(3-(morpholine-4-carbonyl)-[1,4'-bipiperidin]-1'-yl)methanone | (3R)-1'-(9-anthrylcarbonyl)-3-(morpholin-4-ylcarbonyl)-1,4'-bipiperidine | CP640186 | UNII-04L1E4J3ZT | 04L1E4J3ZT | [(3R)-1-[1-(anthra | ||
| CAS number | 591778-68-6 | molecular formula | C30H35N3O3 |
| molecular weight | 485.62 g/mol | Exact mass | - |
| PSA | 53.100 Ų | logp | 2.88 |
numbering system
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physicochemical properties
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激
Statement of Preventive Measures：
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
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MSDS
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