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SKU | Taille | Disponibilité |
Prix | Qté |
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C647539-5mg
|
5mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
90,90$US
|
|
C647539-10mg
|
10mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
144,90$US
|
|
C647539-25mg
|
25mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
300,90$US
|
|
C647539-50mg
|
50mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
480,90$US
|
|
C647539-100mg
|
100mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
768,90$US
|
|
Spécifications et pureté | ≥99% |
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Mécanismes biochimiques et physiologiques | CP-640186 hydrochloride is an orally active and cell-permeable Acetyl-CoA carboxylase ( ACC ) inhibitor with IC 50 s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively. Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty aci |
Température de stockage | Store at 2-8°C,Desiccated |
Expédié en |
Wet ice Ce produit nécessite l'expédition en chaîne froide. Les services terrestres et autres services économiques ne sont pas disponibles. |
Product Description |
CP-640186 hydrochloride is an orally active and cell-permeable Acetyl-CoA carboxylase ( ACC ) inhibitor with IC 50 s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively. Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism that enables the synthesis of malonyl-CoA. CP-640186 hydrochloride can also stimulate muscle fatty acid oxidation In Vitro CP-640186 (20 µM; 48 h) treatment can inhibit H460 cell growth. CP-640186 (0.1 nM-100 µM; 2 h) treatment increases fatty acid metabolism in a concentration-dependent manner in C2C12 cells and muscle strips. CP-640186 (0.62-1.8 µM; 2 h) treatment inhibits fatty acid synthesis and TG synthesis in HepG2 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: Human fibroblasts and H460 cells Concentration: 20 µM Incubation Time: 48 hours Result: Led to a ∼30% decrease in cell number compared to vehicle-treated controls. Cell Viability AssayCell Line: C2C12 cells and muscle strips Concentration: 0.1 nM-100 µM Incubation Time: 2 hours Result: Stimulated palmitate acid oxidation with an EC 50 of 57 nM and a maximal stimulation of 280% in C2C12 cells. Stimulated palmitate acid oxidation with an EC 50 of 1.3 μM and a maximal stimulation of 240% in isolated rat epitrochlearis muscle. Cell Viability AssayCell Line: HepG2 cells Concentration: 0.62-1.8 µM Incubation Time: 6 hours Result: Inhibited fatty acid synthesis and TG synthesis in HepG2 cells with EC 50 s of 0.62 μM and 1.8 μM, respecticely. In Vivo CP-640186 (oral gavage; 4.6-21 mg/kg; once) demonstrates acute efficacy . CP-640186 (intravenous injection and oral gavage; Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg; once) shows lowe drug exposure in the rat than the ob/ob mouse at equal doses . CP-640186 (oral gavage; 100 mg/kg; once) treatment shows a complete shift from carbohydrate utilization to fatty acid utilization as a source of energy at high exposure level . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male ob/ob mice Dosage: 4.6-21 mg/kg Administration: Oral gavage; 4.6-21 mg/kg; once Result: Demonstrated acute efficacy for up to 8 h after oral administration, exhibiting ED 50 values of 4.6, 9.7, and 21 mg/kg, at 1, 4, and 8 h, respectively, after treatment. Animal Model: Male Sprague-Dawley rats Dosage: Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg Administration: Intravenous injection and oral gavage; intravenous dose, 5 mg/kg; oral dose, 10 mg/kg; once Result: Showed a plasma half-life of 1.5 h, a bioavailability of 39%, a Cl p of 65 ml/min/kg, a V dss of 5 liters/kg, an oral T max of 1.0 h, an oral C max of 345 ng/mL, and an oral AUC 0-∞ of 960 ng•h/mL. Animal Model: Male ob/ob mice Dosage: Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg Administration: Intravenous injection and oral gavage; Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg; once Result: Showed a plasma half-life of 1.1 h, a bioavailability of 50%, a Cl p of 54 ml/min/kg, an oral T max of 0.25 h, an oral C max of 2177 ng/mL, and an oral AUC 0-∞ of 3068 ng•h/mL. Animal Model: Twenty male Sprague-Dawley rats (350-400 g) fasted and then refed a high sucrose diet for 2 days; additional eight rats fasted for 24 h Dosage: 100 mg/kg Administration: Oral gavage; 100 mg/kg; once Result: Resulted in time-dependent reductions in RQ (a ratio of CO 2 production to O 2 consumption) of up to 64%. Form:Solid IC50& Target:IC50: 53 nM (rat liver ACC1) and 61 nM (rat skeletal muscle ACC2) |
Taxonomy Tree
Kingdom | Organic compounds |
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Superclass | Benzenoids |
Classe | Anthracenes |
Subclass | Anthracenecarboxylic acids and derivatives |
Intermediate Tree Nodes | Not available |
Direct Parent | Anthracenecarboxylic acids and derivatives |
Alternative Parents | N-benzoylpiperidines Naphthalenecarboxamides Piperidinecarboxamides Aminopiperidines Morpholines Tertiary carboxylic acid amides Trialkylamines Amino acids and derivatives Oxacyclic compounds Dialkyl ethers Azacyclic compounds Organic oxides Hydrochlorides Hydrocarbon derivatives Carbonyl compounds |
Molecular Framework | Aromatic heteropolycyclic compounds |
Substituents | Anthracene carboxylic acid or derivatives - N-benzoylpiperidine - 1-naphthalenecarboxamide - 1-naphthalenecarboxylic acid or derivatives - N-acyl-piperidine - Piperidinecarboxamide - 3-piperidinecarboxamide - 4-aminopiperidine - Morpholine - Piperidine - Oxazinane - Tertiary carboxylic acid amide - Amino acid or derivatives - Carboxamide group - Tertiary aliphatic amine - Tertiary amine - Carboxylic acid derivative - Dialkyl ether - Ether - Oxacycle - Azacycle - Organoheterocyclic compound - Organic oxygen compound - Organic nitrogen compound - Amine - Hydrocarbon derivative - Organic oxide - Hydrochloride - Carbonyl group - Organooxygen compound - Organonitrogen compound - Aromatic heteropolycyclic compound |
Description | This compound belongs to the class of organic compounds known as anthracenecarboxylic acids and derivatives. These are organic compounds containing a carboxylic acid group (or a derivative thereof) attached to an anthracene ring system. |
External Descriptors | Not available |
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IUPAC Name | [(3R)-1-[1-(anthracene-9-carbonyl)piperidin-4-yl]piperidin-3-yl]-morpholin-4-ylmethanone;hydrochloride |
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INCHI | InChI=1S/C30H35N3O3.ClH/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;1H/t24-;/m1./s1 |
InChIKey | DUBNXJIOBFRASV-GJFSDDNBSA-N |
Smiles | C1CC(CN(C1)C2CCN(CC2)C(=O)C3=C4C=CC=CC4=CC5=CC=CC=C53)C(=O)N6CCOCC6.Cl |
Isomères SMILES | C1C[C@H](CN(C1)C2CCN(CC2)C(=O)C3=C4C=CC=CC4=CC5=CC=CC=C53)C(=O)N6CCOCC6.Cl |
PubChem CID | 23589188 |
Poids moléculaire | 522.08 |
Solubilité | H2O : 50 mg/mL (95.77 mM; Need ultrasonic) DMSO : ≥ 48 mg/mL (91.94 mM) |
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Poids moléculaire | 522.100 g/mol |
XLogP3 | |
Hydrogen Bond Donor Count | 1 |
Hydrogen Bond Acceptor Count | 4 |
Rotatable Bond Count | 3 |
Exact Mass | 521.245 Da |
Monoisotopic Mass | 521.245 Da |
Topological Polar Surface Area | 53.100 Ų |
Heavy Atom Count | 37 |
Formal Charge | 0 |
Complexity | 753.000 |
Isotope Atom Count | 0 |
Defined Atom Stereocenter Count | 1 |
Undefined Atom Stereocenter Count | 0 |
Defined Bond Stereocenter Count | 0 |
Undefined Bond Stereocenter Count | 0 |
The total count of all stereochemical bonds | 0 |
Covalently-Bonded Unit Count | 2 |