1,2,5,6-tetrahydro-1-methyl-3-pyridinecarboxylicacid, methyl ester, hydrobromide

Tyrosine407 phosphorylation activates mitochondrial acetyl-CoAacetyltransferase 1 (ACAT1) by stabilizing its tetramer. This is believed to bethe mechanisms by which ACAT1 is “hijacked” and contributes to the Warburgeffect in cancer. Arecoline is a covalent inhibitor of ACAT1 which binds to anddisrupts only ACAT1 tetramers (IC₅₀=11.1 ?M). ACAT2 and DLAT are notinhibited. Treatment of xenograft nude mice with Arecoline resulted in adose-dependent reduction in tumor mass. Agonist at muscarinic acetylcholinereceptors M1 – M5 (EC₅₀ in the range of 7-410 nM). May be effectivein dementia.

Physical Properties:White crystallinepowder

MW=236.1 C₈H₁₃NO₂ • HBr

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

Solubilization: May be dissolved inwater (50 mg/ml)

Storage: Store desiccated assupplied at ambient temperature for up to2 years. Do not store solutions for longer than one day

Amount: 250 mg