SB 204990

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Cat.No. 4962 - SB 204990 | C18H22Cl2O5 | CAS No. 154566-12-8
Description: ATP citrate lyase (ACLY) inhibitor
Chemical Name: (3R,5S)-rel-5-[6-(2,4-Dichlorophenyl)hexyl]tetrahydro-3-hydroxy-2-oxo-3-furanacetic acid
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature

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
ethanol 38.93 100
DMSO 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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the biological activity of the product.

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


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Keywords: SB 204990, SB 204990 supplier, SB204990, ATP-citrate, lyases, ACL, inhibitors, inhibits, prodrug, SB-201076, cholesterol, fatty, acid, metabolic, lipids, synthases, transferases, ACLY, ATP, Citrate, Lyase, 4962, Tocris Bioscience

1 Citation for SB 204990

Citations are publications that use Tocris products. Selected citations for SB 204990 include:

Shah et al (2016) Targeting ACLY sensitizes castration-resistant prostate cancer cells to AR antagonism by impinging on an ACLY-AMPK-AR feedback mechanism. Oncotarget 7 43713 PMID: 27248322


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Literature in this Area

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