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PD 128042

CAT: 0804-HY-107572-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-107572-01Size:5 mg
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Description
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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2

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