Arecoline HBr, ACAT1 inhibitor (TBI1016)

Description

Product Details

Formal Name: 1,2,5,6-Tetrahydro-1-methyl-3-pyridinecarboxylic acid, methyl ester, hydrobromide

Molecular Formula: C₈H₁₃NO₂ HBr

Formula Weight: 236.11

CAS Number: 300-08-3

Purity: >98%

Formulation: powder

Solubility: Soluble in Water (up to 50 mg/ml).

Storage: RT

Stability: ≥ 2 years.

Applications

ACAT1 inhibitor

Functions

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 μM). 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.

Application Procedures

First dissolved in Water (up to 50 mg/ml), then diluted to aqueous buffer. Solutions are not stable – make fresh daily.