PD 128042

PD 128042 (CI 976) is a potent, orally active, and selective inhibitor of ACAT (acyl coenzyme A:cholesterol acyltransferase) with an IC50s of 73 nM. PD 128042 is also a potent LPAT (lysophospholipid acyltransferase) inhibitor. PD 128042 inhibits Golgi-associated LPAT activity (IC50=15 μM) . PD 128042 inhibits multiple membrane trafficking steps, including ones found in the endocytic and secretory pathway[1][2][3].

Product Specifications

CAS Number

[114289-47-3]

Product Name Alternative

CI 976

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Acyltransferase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/pd-128042.html

Concentration

10mM

Purity

99.97

Solubility

DMSO : 100 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CCCCCCCCCCC(C)(C)C(NC1=C(C=C(OC)C=C1OC)OC)=O

Molecular Formula

C23H39NO4

Molecular Weight

393.56

Precautions

H302, H315, H319, H335

References & Citations

[1]Chambers K, et al. A unique lysophospholipid acyltransferase (LPAT) antagonist, CI-976, affects secretory and endocytic membrane trafficking pathways. J Cell Sci. 2005;118 (Pt 14) :3061-3071.|[2]O'Brien PM, et al. Inhibitors of acyl-CoA:cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 8. Incorporation of amide or amine functionalities into a series of disubstituted ureas and carbamates. Effects on ACAT inhibition in vitro and efficacy in vivo. J Med Chem. 1994;37 (12) :1810-1822. |[3]Drecktrah D, et al. Inhibition of a Golgi complex lysophospholipid acyltransferase induces membrane tubule formation and retrograde trafficking. Mol Biol Cell. 2003;14 (8) :3459-3469. |[4]Krause BR, et al. In vivo evidence that the lipid-regulating activity of the ACAT inhibitor CI-976 in rats is due to inhibition of both intestinal and liver ACAT. J Lipid Res. 1993;34 (2) :279-294.