| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| C424935-1ml |
1ml |
现货  |
|
| 英文别名 | 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-(anthracene-9-carbonyl) |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | CP 640186 |
| 生化机理 | CP 640186 是一种同工酶非选择性 ACC（乙酰-CoA 羧化酶）抑制剂，对大鼠肝脏 ACC1 和大鼠骨骼肌 ACC2 的 IC50 值分别为 53 和 61 nM。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 乙酰辅酶羧化酶 1 抑制剂；乙酰辅酶羧化酶 2 抑制剂 |
| 产品介绍 |
说明： 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. |
| ALogP | 2.88 |
|---|---|
| hba_count | 3 |
| Rotatable Bond | 3 |
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 小分子 |
|---|---|
| IIUPAC Name | [(3R)-1-[1-(anthracene-9-carbonyl)piperidin-4-yl]piperidin-3-yl]-morpholin-4-ylmethanone |
| INCHI | 1S/C30H35N3O3/c34-29(32-16-18-36-19-17-32)24-8-5-13-33(21-24)25-11-14-31(15-12-25)30(35)28-26-9-3-1-6-22(26)20-23-7-2-4-10-27(23)28/h1-4,6-7,9-10,20,24-25H,5,8,11-19,21H2/t24-/m1/s1 |
| InChi Key | LDQKDRLEMKIYMC-XMMPIXPASA-N |
| Smiles | C1CC(CN(C1)C2CCN(CC2)C(=O)C3=C4C=CC=CC4=CC5=CC=CC=C53)C(=O)N6CCOCC6 |
| Isomeric SMILES | C1C[C@H](CN(C1)C2CCN(CC2)C(=O)C3=C4C=CC=CC4=CC5=CC=CC=C53)C(=O)N6CCOCC6 |
| 分子量 | 485.62 |
| Reaxy-Rn | 14183663 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=14183663&ln= |
| DMSO(mg / mL) Max Solubility | 97 |
|---|---|
| DMSO(mM) Max Solubility | 199.744656315638 |
| Water(mg / mL) Max Solubility | ＜1 |
| 分子量 | 485.600 g/mol |
| XLogP3 | 4.100 |
| 氢键供体数Hydrogen Bond Donor Count | 0 |
| 氢键受体数Hydrogen Bond Acceptor Count | 4 |
| 可旋转键计数Rotatable Bond Count | 3 |
| 精确质量Exact Mass | 485.268 Da |
| 单同位素质量Monoisotopic Mass | 485.268 Da |
| 拓扑极表面积Topological Polar Surface Area | 53.100 Ų |
| 重原子数Heavy Atom Count | 36 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 753.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 1 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
| 象形图 | GHS07 |
|---|---|
| 信号词 | 警告 |
| 危险声明 |
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 |
| 预防措施声明 |
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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