SB 204990

ATP citrate lyase (ACLY) inhibitor CAS# 154566-12-8

SB 204990

Catalog No. BCC6342----Order now to get a substantial discount!

Product Name & Size Price Stock
SB 204990: 5mg $138 In Stock
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Quality Control of SB 204990

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Chemical structure

SB 204990

3D structure

Chemical Properties of SB 204990

Cas No. 154566-12-8 SDF Download SDF
PubChem ID 132975 Appearance Powder
Formula C18H22Cl2O5 M.Wt 389.27
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 250 mg/mL (642.23 mM; Need ultrasonic)
H2O : 10 mg/mL (25.69 mM; Need ultrasonic)
Chemical Name (2R)-2-[(2S)-8-(2,4-dichlorophenyl)-2-hydroxyoctyl]-2-hydroxybutanedioic acid
SMILES C1=CC(=C(C=C1Cl)Cl)CCCCCCC(CC(CC(=O)O)(C(=O)O)O)O
Standard InChIKey NPZOIISFQXTCQN-KBXCAEBGSA-N
Standard InChI InChI=1S/C18H24Cl2O6/c19-13-8-7-12(15(20)9-13)5-3-1-2-4-6-14(21)10-18(26,17(24)25)11-16(22)23/h7-9,14,21,26H,1-6,10-11H2,(H,22,23)(H,24,25)/t14-,18+/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of SB 204990

DescriptionATP 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.

SB 204990 Dilution Calculator

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SB 204990 Molarity Calculator

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Preparing Stock Solutions of SB 204990

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.5689 mL 12.8446 mL 25.6891 mL 51.3782 mL 64.2228 mL
5 mM 0.5138 mL 2.5689 mL 5.1378 mL 10.2756 mL 12.8446 mL
10 mM 0.2569 mL 1.2845 mL 2.5689 mL 5.1378 mL 6.4223 mL
50 mM 0.0514 mL 0.2569 mL 0.5138 mL 1.0276 mL 1.2845 mL
100 mM 0.0257 mL 0.1284 mL 0.2569 mL 0.5138 mL 0.6422 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on SB 204990

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.[Pubmed:9693110]

Biochem J. 1998 Aug 15;334 ( Pt 1):113-9.

ATP citrate (pro-S)-lyase (EC 4.1.3.8), a cytosolic enzyme that generates acetyl-CoA for cholesterol and fatty acid synthesis de novo, is a potential target for hypolipidaemic intervention. Here we describe the biological effects of the inhibition of ATP citrate-lyase on lipid metabolism in Hep G2 cells, and plasma lipids in rats and dogs, by using SB-204990, the cell-penetrant gamma-lactone prodrug of the potent ATP citrate-lyase inhibitor SB-201076 (Ki=1 microM). Consistent with an important role of ATP citrate-lyase in the supply of acetyl-CoA units for lipid synthesis de novo, SB-204990 inhibited cholesterol synthesis and fatty acid synthesis in Hep G2 cells (dose-related inhibition of up to 91% and 82% respectively) and rats (76% and 39% respectively). SB-204990, when administered orally to rats, was absorbed into the systemic circulation; pharmacologically relevant concentrations of SB-201076 were recovered in the liver. When administered in the diet (0.05-0. 25%, w/w) for 1 week, SB-204990 caused a dose-related decrease in plasma cholesterol (by up to 46%) and triglyceride levels (by up to 80%) in rats. This hypolipidaemic effect could be explained, at least in part, by a decrease (up to 48%) in hepatic very-low-density lipoprotein (VLDL) production as measured by the accumulation of VLDL in plasma after injection of Triton WR-1339. SB-204990 (25 mg/kg per day) also decreased plasma cholesterol levels (by up to 23%) and triglyceride levels (by up to 38%) in the dog, preferentially decreasing low-density lipoprotein compared with high-density lipoprotein cholesterol levels. Overall these results are consistent with the concept that ATP citrate-lyase is an important enzyme in controlling substrate supply for lipid synthesis de novo and a potential enzyme target for hypolipidaemic intervention.

ATP-Citrate lyase as a target for hypolipidemic intervention. 2. Synthesis and evaluation of (3R,5S)-omega-substituted-3-carboxy-3, 5-dihydroxyalkanoic acids and their gamma-lactone prodrugs as inhibitors of the enzyme in vitro and in vivo.[Pubmed:9733484]

J Med Chem. 1998 Sep 10;41(19):3582-95.

A series of (3R,5S)-omega-substituted-3-carboxy-3, 5-dihydroxyalkanoic acids have been synthesized and evaluated as inhibitors of the recombinant human form of ATP-citrate lyase. The best of these have Ki's in the 200-1000 nM range. As the corresponding thermodynamically favored gamma-lactone prodrugs, a number of compounds are able to inhibit cholesterol and fatty acid synthesis in HepG2 cells and reduce plasma triglyceride levels in vivo. The best of these, compound 77, is able to induce clear hypocholesterolemic and hypotriglyceridaemic responses when administered orally to rat and dog. These results provide evidence to support the hypothesis that compounds which inhibit ATP-citrate lyase have the potential to be a novel class of hypolipidemic agent, which possess combined hypocholesterolemic and hypotriglyceridemic activities.

Description

SB 204990 is a potent and specific inhibitor of ATP citrate lyase (ACLY) enzyme.

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