PD 128042
Based on 1 publication(s) in Google Scholar
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.
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- Reinheit: 99.97%
- CAS. Nr.: 114289-47-3
- Formel: C23H39NO4
- Molecular Weight:393.56
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Orally Active Compound Library
HY-L061
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Lipid Metabolism Compound Library
HY-L091
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Human Metabolite Library
HY-L123
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HY-L158
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Publications Citing Use of MedChemExpress (MCE) PD 128042
More
Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | IC50 |
838 nM
Compound: Cl-976
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Compound was tested for inhibitory activity against ACAT from Caco-2 microsome in human
Compound was tested for inhibitory activity against ACAT from Caco-2 microsome in human
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[PMID: 10450977] |
| Huh-7 | EC50 |
0.6 μM
Compound: CI-976
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Induction of ABCA1 mRNA expression in human HuH7 cells after 24 hrs
Induction of ABCA1 mRNA expression in human HuH7 cells after 24 hrs
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[PMID: 23025824] |
| Peritoneal macrophage | IC50 |
3.8 μM
Compound: 4; CI-976
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Inhibition of formation of foam cells in rat peritoneal macrophages
Inhibition of formation of foam cells in rat peritoneal macrophages
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[PMID: 36473091] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 114289-47-3
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Appearance Solid
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Molecular Weight 393.56
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Formel C23H39NO4
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Color White to off-white
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SMILES
CCCCCCCCCCC(C)(C)C(NC1=C(C=C(OC)C=C1OC)OC)=O
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Synonyms
CI 976
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Aquat Toxicol
Is acyl-CoA cholesterol acyltransferase 2 the enzyme responsible for the esterification of okadaic acid in bivalves?. [Abstract]2026 Jun:295:107814. PMID: 41935504
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (254.09 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (269 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5409 mL | 12.7045 mL | 25.4091 mL | 63.5227 mL |
| 5 mM | 0.5082 mL | 2.5409 mL | 5.0818 mL | 12.7045 mL | |
| 10 mM | 0.2541 mL | 1.2705 mL | 2.5409 mL | 6.3523 mL | |
| 15 mM | 0.1694 mL | 0.8470 mL | 1.6939 mL | 4.2348 mL | |
| 20 mM | 0.1270 mL | 0.6352 mL | 1.2705 mL | 3.1761 mL | |
| 25 mM | 0.1016 mL | 0.5082 mL | 1.0164 mL | 2.5409 mL | |
| 30 mM | 0.0847 mL | 0.4235 mL | 0.8470 mL | 2.1174 mL | |
| 40 mM | 0.0635 mL | 0.3176 mL | 0.6352 mL | 1.5881 mL | |
| 50 mM | 0.0508 mL | 0.2541 mL | 0.5082 mL | 1.2705 mL | |
| 60 mM | 0.0423 mL | 0.2117 mL | 0.4235 mL | 1.0587 mL | |
| 80 mM | 0.0318 mL | 0.1588 mL | 0.3176 mL | 0.7940 mL | |
| 100 mM | 0.0254 mL | 0.1270 mL | 0.2541 mL | 0.6352 mL |
PD 128042 Related Classifications
HY-107572 Related Classifications
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