Biological Activity
ATP citrate lyase (ACLY) inhibitor. Prodrug of SB 201076. Inhibits cholesterol and fatty acid synthesis in a dose-dependent manner in HepG2 cells. Orally active in vivo.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Technical Data
| M. Wt | 389.27 |
| Formula | C18H22Cl2O5 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 154566-12-8 |
| PubChem ID | 10340264 |
| InChI Key | YTRNLFYTHYWDAU-KDOFPFPSSA-N |
| Smiles | ClC(C=C(Cl)C=C2)=C2CCCCCC[C@@H](OC1=O)C[C@]1(O)CC(O)=O |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.93 | 100 | |
| ethanol | 38.93 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 389.27. 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 | 2.57 mL | 12.84 mL | 25.69 mL |
| 5 mM | 0.51 mL | 2.57 mL | 5.14 mL |
| 10 mM | 0.26 mL | 1.28 mL | 2.57 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.51 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Pearce et al (1998) The role of ATP citrate-lyase in the metabolic regulation of plasma lipids. Hypolipidaemic effects of SB-204990, a lactone prodrug of the potent ATP citrate-lyase inhibitor SB-201076. Biochem.J. 334 113 PMID: 9693110
Gribble et al (1998) ATP-Citrate lyase as a target for hypolipidemic intervention. 2. Synthesis and evaluation of (3R*,5S*)-ω-substituted-3-carboxy-3, 5-dihydroxyalkanoic acids and their gamma-lactone prodrugs as inhibitors of the enzy J.Med.Chem. 41 3582 PMID: 9733484
Keywords: SB 204990, supplier, SB204990, ATP-citrate, lyases, ACL, inhibitors, inhibits, prodrug, SB-201076, cholesterol, fatty, acid, metabolic, lipids, synthases, transferases, ACLY, ATP, Citrate, Lyase, ATP, Citrate, Lyase, Tocris Bioscience
