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Product Details

Arecoline HBr | ACAT1 inhibitor

Arecoline (300-8-3) is a covalent inhibitor of ACAT1 which binds to and disrupts only ACAT1 tetramers (IC50=11.1 μM). ACAT2 and DLAT are not inhibited. 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.  Treatment of xenograft nude mice with Arecoline resulted in a dose-dependent reduction in tumor mass.1 Agonist at muscarinic acetylcholine receptors M1 – M5 (EC50 in the range of 7-410 nM).2 May be effective in dementia.3

References/Citations

1) Fan et al. (2016), Tetrameric Acetyl-CoA Acetyltransferase 1 is Important for Tumor Growth; Mol. Cell, 64 859
2) Heinrich et al. (2009), Pharmacological comparison of muscarinic ligands: historical versus more recent muscarinic M1-preferring receptor agonists; Eur. J. Pharmacol., 605 53
3) Christie et al. (1981), Physostigmine and arecoline: effects of intravenous infusions in Alzheimer presenile dementia; Br. J. Psychiatry, 138 46

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Catalog#  10-1016-0250

$30.00
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Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
300.08-3
Catalog Number:
10-1016
Activity:
ACAT1 inhibitor
Chemical Name:
1,2,5,6-Tetrahydro-1-methyl-3-pyridinecarboxylic acid, methyl ester, hydrobromide
Molecular Weight:
236.11
Molecular Formula:
C8H13NO2 HBr
Solubility:
Soluble in Water (up to 50 mg/ml)
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT (des.)
Stability:
Stable for one year as supplied. Solutions in distilled water are not stable and should not be stored. Make fresh solutions daily.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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