Selective acyl-coenzyme A:cholesterol acyltransferase (ACAT) inhibitor (IC50 = 0.073 μM). Lowers non-high density lipoprotein (HDL)-cholesterol and increases HDL-cholesterol concentrations in rats with pre-established dyslipidemia. Orally active. Also inhibits Golgi-associated LPL acyltransferase (LPAT) activity (IC50 = 15 μM).
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 393.57. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.54 mL||12.7 mL||25.41 mL|
|5 mM||0.51 mL||2.54 mL||5.08 mL|
|10 mM||0.25 mL||1.27 mL||2.54 mL|
|50 mM||0.05 mL||0.25 mL||0.51 mL|
References are publications that support the biological activity of the product.
Krause et al (1993) In vivo evidence that the lipid-regulating activity of ACAT inhibitor CI-976 in rats is due to inhibition of both intestinal and liver ACAT. J.Lipid Res. 34 279 PMID: 8429262
Sliskovic and White (1991) Therapeutic potential of ACAT inhibitors as lipid lowering and anti-atherosclerotic agents. TiPS. 12 194
Drecktrah et al (2003) Inhibition of a Golgi complex lysophospholipid acyltransferase induces membrane tubule formation and retrograde trafficking. Mol.Biol.Cell 14 3549
If you know of a relevant reference for CI 976, please let us know.
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Keywords: CI 976, CI 976 supplier, Acyl-CoAcholesterol, acyltransferase, ACAT, inhibitors, inhibits, Transferases, CI976, Acyl-CoA:Cholesterol, Acyltransferase, 2227, Tocris Bioscience
2 Citations for CI 976
Citations are publications that use Tocris products. Selected citations for CI 976 include:
Pagliuso et al (2016) Golgi membrane fission requires the CtBP1-S/BARS-induced activation of lysophosphatidic acid acyltransferase δ Nature Communications 7 12148 PMID: 27401954
Schmidt and Brown (2009) Lysophosphatidic acid acyltransferase 3 regulates Golgi complex structure and function. J Cell Biol 186 211 PMID: 19635840
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Literature in this Area
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Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.