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SB 204990
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SB 204990图片
CAS NO:154566-12-8
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍

化学性质

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
Canonical SMILESClC1=CC(Cl)=C(C=C1)CCCCCC[C@](O2)([H])C[C@](C2=O)(O)CC(O)=O
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

资料参考

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.

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.