JavaScript seems to be disabled in your browser. For the best experience on our site, be sure to turn on Javascript in your browser.
Tel: +1-832-696-8203
Email: [email protected]
Worldwide Distributors
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
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 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
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.