Inhibitor of carnitine palmitoyltransferases
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Perhexiline (maleate)

Item No. 16982

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(2,2-dicyclohexylethyl)-piperidine, 2Z-butenedioate
CAS Number
6724-53-4
Molecular Formula
C19H35N • C4H4O4
Formula Weight
393.6
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 5 mg/ml
λmax
210 nm
SMILES
OC(/C=C\C(O)=O)=O.C1(CC(C2CCCCC2)C3CCCCC3)NCCCC1
InChi Code
InChI=1S/C19H35N.C4H4O4/c1-3-9-16(10-4-1)19(17-11-5-2-6-12-17)15-18-13-7-8-14-20-18;5-3(6)1-2-4(7)8/h16-20H,1-15H2;1-2H,(H,5,6)(H,7,8)/b;2-1-
InChi Key
JDZOTSLZMQDFLG-BTJKTKAUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Perhexiline is a carnitine palmitoyltransferase 1 (CPT1) and CPT2 inhibitor that was originally developed as an anti-anginal drug in the 1970s.1,2,3 It inhibits rat heart and liver CPT1 (IC50 = 77 and 148 µM, respectively) and rat heart CPT2 (IC50 = 79 µM).1,2 Inhibition of CPT reduces uptake of long-chain fatty acids into the mitochondria, thereby shifting cellular metabolism from β-oxidation to glycolysis. Perhexilin inhibits mTORC1 signaling at 10 µM and induces autophagy ~7-fold at a concentration of 10 µM in MCF-7 cells.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kennedy, J.A., Unger, S.A., and Horowitz, J.D. Inhibition of carnitine palmitoyltransferase-1 in rat heart and liver by perhexiline and amiodarone. Biochem. Pharmacol. 52(2), 273-280 (1996).

    2. Kennedy, J.A., Kiosoglous, A.J., Murphy, G.A., et al. Effect of perhexiline and oxfenicine on myocardial function and metabolism during low-flow ischemia/reperfusion in the isolated rat heart. J. Cardiovasc. Pharmacol. 36(6), 794-801 (2000).

    3. Ashrafian, H., Horowitz, J.D., and Frenneaux, M.P. Perhexiline. Cardiovasc. Drug Rev. 25(1), 76-97 (2007).

    4. Balgi, A.D., Fonseca, B.D., Donohue, E., et al. Screen for chemical modulators of autophagy reveals novel therapeutic inhibitors of mTORC1 signaling. PLoS One 4(9), e7124 (2009).

    Product Citations

    Xu, S., Catapang, A., Braas, D., et al. A precision therapeutic strategy for hexokinase 1-null, hexokinase 2-positive cancers. Cancer & Metab. 6:7, (2018).