5.33978

ACC Inhibitor IV, CP-640186

• 別名: ACC Inhibitor IV, CP-640186, 9-Anthryl((3 R)-3-(4-morpholinylcarbonyl)-1,4ʹ-bipiperidin-1ʹ-yl)methanone, HCl, Acetyl-CoA Carboxylase Inhibitor IV, CP-640186, HCl
• 実験式（ヒル表記法）: C₃₀H₃₅N₃O₃
• 分子量: 485.62
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• アッセイ: ≥98% (HPLC)
• 品質水準: 100
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; desiccated (hygroscopic); protect from light
• 色: light orange
• 溶解性: DMSO: 50 mg/mL; H₂O: 50 mg/mL
• 保管温度: 2-8°C

詳細

詳細

A cell-permeable, orally active, non-toxic bipiperidylcarboxamide derived compound that binds to the active site of acetyl-CoA carboxylase (ACC) at the interface between the two monomers of the CT dimer and acts as a potent, allosteric, and reversible, inhibitor of ACC (IC₅₀ = 53 nM and 61 nM for rat liver ACC1 and ACC2). The inhibition is uncompetitive with respect to ATP and non-competitive with respect to acetyl-CoA, citrate, and bicarbonate. Shown to inhibit fatty acid synthesis in Sprague-Dawley rats, and in CD1 and ob/ob mice (ED₅₀ = 13, 11, and 4 mg/kg). Stimulates fatty acid oxidation in CC12 cells in rat epitrochelearis muscle (ED₅₀ = 57 nM) and reduces muscle malonyl-CoA levels. Improves insulin sensitivity in diet-induced obese animal models. Displays good metabolic stability and moderate pharmacokinetic properties (plasma half-life =1.5 h; C_max = 345 ng/ml; and AUC = 960 ng/h/ml at 5 mg/kg i.v. or 10 mg/kg p.o.).

ACC Inhibitor IV, CP-640186, is a cell-permeable, potent, allosteric, eversible inhibitor of ACC (IC₅₀ = 53 and 61 nM for rat liver ACC1 & ACC2). The inhibition is uncompetitive with respect to ATP.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
Acetyl-CoA carboxylase (ACC)

Target IC₅₀: 53 nM and 61 nM for rat liver ACC1 and ACC2

警告

Toxicity: Standard Handling (A)

物理的形状

Supplied as a hydrochloride salt.

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

その他情報

Tong, L., and Harwood, H.J., 2006. J. Cell. Biol.99, 1476.
Gu, Y.G., et al. 2006. J. Med. Chem.49, 3770.

Zhang, H., et al. 2004. Structure12, 1683.

Harwood, H.J., et al. 2003. J. Biol. Chem.278, 37099.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3