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PD 128042

Catalog No. T22665   CAS 114289-47-3
Synonyms: CI 976

PD 128042 (CI 976) is a potent orally active and selective ACAT inhibitor(IC50: 73 nM) and a potent lysophospholipid acyltransferase(LPAT) inhibitor. CI 976 inhibits Golgi-associated LPAT activity (IC50: 15 μM) and multiple membrane trafficking steps.

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PD 128042 Chemical Structure
PD 128042, CAS 114289-47-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 43.00
2 mg In stock $ 61.00
5 mg In stock $ 87.00
10 mg In stock $ 129.00
25 mg In stock $ 279.00
50 mg In stock $ 519.00
100 mg In stock $ 752.00
1 mL * 10 mM (in DMSO) In stock $ 98.00
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Purity: 99.44%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PD 128042 (CI 976) is a potent orally active and selective ACAT inhibitor(IC50: 73 nM) and a potent lysophospholipid acyltransferase(LPAT) inhibitor. CI 976 inhibits Golgi-associated LPAT activity (IC50: 15 μM) and multiple membrane trafficking steps.
Targets&IC50 Golgi-associated LPAT:15 μM, ACAT:73 nM
In vitro In the chronic cholesterol-fed rat model, CI 976 decreases non-high density lipoprotein (HDL)-cholesterol and increases HDL-cholesterol in rats with pre-established dyslipidemia[4].
Synonyms CI 976
Molecular Weight 393.56
Formula C23H39NO4
CAS No. 114289-47-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 25 mg/ml(63.52 mM)

DMF: 25 mg/ml(63.52 mM)

Ethanol: 25 mg/ml(63.52 mM)

TargetMolReferences and Literature

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.

TargetMolCitations

1. Luo W, Chen L, Sun H, et al.Soat2 inhibitor avasimibe alleviates acute pancreatitis by suppressing acinar cell ferroptosis.Naunyn-Schmiedeberg's Archives of Pharmacology.2024: 1-11.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Metabolism Compound Library Lipid Metabolism Compound Library ReFRAME Related Library Bioactive Compound Library Orally Active Compound Library Bioactive Compounds Library Max

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Keywords

PD 128042 114289-47-3 Metabolism Acyltransferase CI 976 inhibit oral CI-976 Diacylglycerol acyltransferase transferase secretory PD128042 LPAT PD-128042 acyl-CoA:cholesterol acyltransferase mono- acylglycerol acyltransferase endocytic membrane trafficking pathway ACAT CI976 Diglyceride acyltransferase Inhibitor inhibitor

 

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