1,2,5,6-tetrahydro-1-methyl-3-pyridinecarboxylic acid, methyl ester, hydrobromide

Tyrosine407 phosphorylation activates mitochondrial acetyl-CoA acetyltransferase 1 (ACAT1) by stabilizing its tetramer. This is believed to be the mechanisms by which ACAT1 is “hijacked” and contributes to the Warburg effect in cancer. Arecoline is a covalent inhibitor of ACAT1 which binds to and disrupts only ACAT1 tetramers (IC₅₀=11.1 ?M). ACAT2 and DLAT are not inhibited. Treatment of xenograft nude mice with Arecoline resulted in a dose-dependent reduction in tumor mass. Agonist at muscarinic acetylcholine receptors M1 – M5 (EC₅₀ in the range of 7-410 nM). May be effective in dementia.

Physical Properties: White crystalline powder

MW= 236.1 C₈H₁₃NO₂• HBr

Analysis: >98% (TLC); NMR (Conforms)

Solubilization: May be dissolved in water (50 mg/ml)

Storage: Store desiccated as supplied at ambient temperature for up to 2 years. Do not store solutions for longer than one day

Amount: 250 mg