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SB 204990

 
Catalog No.
B5782
ATP柠檬酸裂解酶(ACLY)抑制剂
组合的产品项目
规格价格库存 数量
1mg
¥ 590.00
现货
5mg
¥ 1,727.00
现货
10mg
¥ 2,590.00
现货

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A

背景

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

In HepG2 cells, SB 204990 inhibits fatty acid and cholesterol synthesis in a concentration-dependent manner. Oral administration of SB 204990 (25 mg/kg) reduces plasma levels of the lipoproteins VLDL, LDL, and HDL by 21, 40, and 22%, respectively, in dogs. It also reduces VLDL synthesis and plasma cholesterol and triglyceride levels in rats in a dose-dependent manner.

Reference:

[1]. Pearce N J, Yates J W, Berkhout T A, et al. 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, 1998,  334(1): 113-119.

化学属性

Physical AppearanceWhite solid
StorageStore at -20°C
M.Wt389.27
Cas No.154566-12-8
FormulaC18H22Cl2O5
Solubilityinsoluble in H2O; ≥51.2 mg/mL in DMSO; ≥59.4 mg/mL in EtOH
Chemical Name2-((3S,5R)-5-(6-(2,4-dichlorophenyl)hexyl)-3-hydroxy-2-oxotetrahydrofuran-3-yl)acetic acid
SDFDownload SDF
Canonical SMILESClC1=CC(Cl)=C(C=C1)CCCCCC[C@](O2)([H])C[C@](C2=O)(O)CC(O)=O
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试验操作

Cell experiment:[1]

Cell lines

Hep G2 cells

Reaction Conditions

0 ~ 30 μM SB 204990 for 2.5 h incubation

Applications

SB 204990 caused a dose-dependent decrease in the rates of cholesterol and fatty acid synthesis in Hep G2 cells, measured by the incorporation of 3H into the sterol and fatty acid fractions of saponifiable cell lipids during a 2.5 h incubation. At 30 μM SB 204990, decreases in the rates of cholesterol and fatty acid synthesis were 91% and 82%, respectively.

Animal experiment:[1]

Animal models

Male beagle dogs

Dosage form

10 mg/kg per day for 7 days, followed by 25 mg/kg per day for an additional 15 days

Once daily by oral route

Applications

SB 204990, administered at 25 mg/kg for 15 days (after a 7-day starting period at a dose of 10 mg/kg), caused a significant and sustained decrease in fasting plasma cholesterol and triglyceride levels of up to 23%and 38%, respectively. SB 204990 significantly decreased cholesterol levels in the LDL and HDL fractions, with the effects on LDL being proportionately the greatest.

Note

The technical data provided above is for reference only.

References:

1. Pearce NJ, Yates JW, Berkhout TA, et al. 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. Biochemical Journal, 1998, 334 (1):113-119.

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