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CP-640186

Names

[ CAS No. ]:
591778-68-6

[ Name ]:
CP-640186

[Synonym ]:
Methanone, 9-anthracenyl[(3R)-3-(4-morpholinylcarbonyl)[1,4'-bipiperidin]-1'-yl]-
9-Anthryl[(3R)-3-(4-morpholinylcarbonyl)-1,4'-bipiperidin-1'-yl]methanone
1w2x
UNII-04L1E4J3ZT
RCP
CP 640186
CP-640186

Biological Activity

[Description]:

CP-640186 is an isozyme-nonselective acetyl-CoA carboxylase (ACCase) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively; with improved metabolic stability vs CP-610431.IC50 value: 53 nM/61 nM (rat liver ACC1/skeletal muscle ACC2) [1]Target: acetyl-CoA carboxylasein vitro: CP-640186, also inhibited both isozymes with IC50s of ~55 nM but was 2–3 times more potent than CP-610431 in inhibiting HepG2 cell fatty acid and TG synthesis. CP-640186 also stimulated fatty acid oxidation in C2C12 cells (ACC2) and in rat epitrochlearis muscle strips with EC50s of 57 nM and 1.3 uM [1]. in vivo: In rats, CP-640186 lowered hepatic, soleus muscle,quadriceps muscle, and cardiac muscle malonyl-CoAwith 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, andstimulated rat whole body fatty acid oxidation with anED50 of ~30 mg/kg [1].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Acetyl-CoA Carboxylase
Research Areas >> Metabolic Disease

[References]

[1]. Harwood HJ Jr, et al. Isozyme-nonselective N-substituted bipiperidylcarboxamide acetyl-CoA carboxylase inhibitors reduce tissue malonyl-CoA concentrations, inhibit fatty acid synthesis, and increase fatty acid oxidation in cultured cells and in experimental animals. J Biol Chem. 2003 Sep 26;278(39):37099-111.

[2]. Yamashita T, et al. Design, synthesis, and structure-activity relationships of spirolactones bearing 2-ureidobenzothiophene as acetyl-CoA carboxylases inhibitors. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6314-8.


[Related Small Molecules]

ND-630 | ND-646 | TOFA | CP-640186 hydrochloride | PF 05175157 | Olumacostat glasaretil | MK-4074

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
721.1±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C30H35N3O3

[ Molecular Weight ]:
485.617

[ Flash Point ]:
389.9±32.9 °C

[ Exact Mass ]:
485.267853

[ PSA ]:
53.09000

[ LogP ]:
3.49

[ Vapour Pressure ]:
0.0±2.3 mmHg at 25°C

[ Index of Refraction ]:
1.654

[ Storage condition ]:
-20℃


Related Compounds