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533978 ACC Inhibitor IV, CP-640186 - Calbiochem

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.

ACC Inhibitor IV, CP-640186 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 9-Anthryl((3R)-3-(4-morpholinylcarbonyl)-1,4ʹ-bipiperidin-1ʹ-yl)methanone, HCl, Acetyl-CoA Carboxylase Inhibitor IV, CP-640186, HCl

Primary Target: Acetyl-CoA carboxylase (ACC)
533978
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Áttekintés

Replacement Information

Kulcsspecifikációk táblázata

Empirical Formula
C₃₀H₃₅N₃O₃

Products

KatalógusszámCsomagolás Menny./csomag
5.33978.0001 Üvegpalack 5 mg
Description
OverviewA 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; Cmax = 345 ng/ml; and AUC = 960 ng/h/ml at 5 mg/kg i.v. or 10 mg/kg p.o.).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Catalogue Number533978
Brand Family Calbiochem®
Synonyms9-Anthryl((3R)-3-(4-morpholinylcarbonyl)-1,4ʹ-bipiperidin-1ʹ-yl)methanone, HCl, Acetyl-CoA Carboxylase Inhibitor IV, CP-640186, HCl
References
ReferencesTong, 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. Structure 12, 1683.
Harwood, H.J., et al. 2003. J. Biol. Chem. 278, 37099.
Product Information
FormLight orange solid
FormulationSupplied as a hydrochloride salt.
Hill FormulaC₃₀H₃₅N₃O₃
Chemical formulaC₃₀H₃₅N₃O₃
Hygroscopic Hygroscopic
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary TargetAcetyl-CoA carboxylase (ACC)
Primary Target IC<sub>50</sub>53 nM and 61 nM for rat liver ACC1 and ACC2
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Katalógusszám GTIN
5.33978.0001 04055977281705

Documentation

ACC Inhibitor IV, CP-640186 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

ACC Inhibitor IV, CP-640186 - Calbiochem Certificates of Analysis

TitleLot Number
533978

References

Hivatkozások áttekintése
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. Structure 12, 1683.
Harwood, H.J., et al. 2003. J. Biol. Chem. 278, 37099.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision20-November-2015 JSW
Synonyms9-Anthryl((3R)-3-(4-morpholinylcarbonyl)-1,4ʹ-bipiperidin-1ʹ-yl)methanone, HCl, Acetyl-CoA Carboxylase Inhibitor IV, CP-640186, HCl
DescriptionA 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; Cmax = 345 ng/ml; and AUC = 960 ng/h/ml at 5 mg/kg i.v. or 10 mg/kg p.o.).
FormLight orange solid
FormulationSupplied as a hydrochloride salt.
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₃₀H₃₅N₃O₃
Purity≥98% by HPLC
SolubilityDMSO (50 mg/ml) or H₂O (50 mg/ml)
Storage Protect from light
+2°C to +8°C
Hygroscopic
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesTong, 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. Structure 12, 1683.
Harwood, H.J., et al. 2003. J. Biol. Chem. 278, 37099.