1. CP-610431

CP-610431 is a reversible, ATP-uncompetitive, isozyme-nonselective acetyl-CoA carboxylase (ACC) inhibitor. CP-610431 inhibits ACC1 and ACC2 with IC50s of ~50 nM. CP-610431 can be used for the research of metabolic syndrome.

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CP-610431 Chemical Structure

CP-610431 Chemical Structure

CAS No. : 591778-83-5

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Description

CP-610431 is a reversible, ATP-uncompetitive, isozyme-nonselective acetyl-CoA carboxylase (ACC) inhibitor. CP-610431 inhibits ACC1 and ACC2 with IC50s of ~50 nM. CP-610431 can be used for the research of metabolic syndrome[1].

In Vitro

CP-610431 is the active R-enantiomer of CP-497485. CP-610431 is more potent than the racemate CP-497485 in inhibiting rat ACC1 (IC50=35.7 nM) and ACC2 (IC50=55 nM), whereas the S-enantiomer, CP-610432, does not substantially inhibit either ACC isoform at concentrations of up to 3 μM. CP-610431 is more potent than CP-497485 in inhibiting HepG2 cell fatty acid and triglyceride (TG) synthesis and in inhibiting TG and apoB secretion[1].
CP-610431 inhibits fatty acid synthesis, triglyceride 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[1].
CP-610431 inhibits both liver and skeletal muscle ACC activity from all three species with essentially equal potency (rat, 36 versus 55 nM; mouse, 50 versus 63 nM; cynomolgus macaque, 70 versus 26 nM) [1].
CP-610431 inhibits mouse primary hepatocyte fatty acid and TG synthesis with IC50 values of 0.11 and 1.2 μM and inhibits TG secretion with an IC50 of 10 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HepG2 cells
Concentration: 0.1, 1, 10 μM
Incubation Time: 24 hours
Result: Dose-dependently inhibited HepG2 cell fatty acid synthesis with an IC50 of 1.6 μM, TG synthesis with an IC50 of 1.8 μM, TG secretion with an IC50 of 3.0 μM, and apoB secretion with an IC50 of 5.7 μM.
In Vivo

CP-610431 inhibits fatty acid synthesis in CD1 mice and ob/ob mice within 1 h after dose with ED50s of 22 and 4 mg/kg, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CD1 mice[1]
Dosage: 30 and 100 mg/kg for fasting CD1 mice; 10, 30, and 100 mg/kg for non-fasting CD1 mice
Administration: Intraperitoneal administration; 1 hour
Result: Inhibited hepatic fatty acid synthesis in fasting CD1 mice by 64±12%, and 77±4% at doses of 30 and 100 mg/kg, respectively.
Inhibited hepatic fatty acid synthesis in non-fasting CD1 mice by 18%, 51%, and 75% at doses of 10, 30 and 100 mg/kg, respectively.
Molecular Weight

471.63

Formula

C30H37N3O2

CAS No.
SMILES

O=C([C@H]1CN(C2CCN(C(C3=C4C=CC=CC4=CC5=CC=CC=C35)=O)CC2)CCC1)N(CC)CC

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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CP-610431
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