Holiday Notification: Cayman Chemical will be closed Monday, May 28, 2012, in observance of the Memorial Day holiday.
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Hormone sensitive lipase (HSL) catalyzes the hydrolysis of tri-, di-, and monoacylglycerols, as well as cholesterol esters, thus mobilizing fatty acids as a primary source of energy in mammals.1 The enzyme is highly expressed in adipose tissue and steroidogenic tissues, and less abundantly in skeletal muscle, heart, brain, pancreatic beta cells, adrenal gland, ovaries, testes, and macrophages. Its presence in various tissues indicates the enzyme plays diverse roles including those in steroidogenesis and spermatogenesis, foam cell formation in atherosclerosis, and diabetes.1,2 CAY10499 is a potent inhibitor of human HSL exhibiting an IC50 of 90 nM for the recombinant enzyme.3 The in vivo pharmacological efficacy of CAY10499 has not been reported.
1
Saltiel, A.R. Another hormone-sensitive triglyceride lipase in fat cells. Proc Natl Acad Sci USA97(2)535-537(2000 Jan 18).
2
Kraemer, F.B., and Shen, W. Hormone-sensitive lipase: Control of intracellular tri-(di-)acylglycerol and cholesteryl ester hydrolysis. J Lipid Res431585-1594(2002 Jan 1).
3
Ali, Y.B., Müller, G., Petry, S., et al. Kinetic characterization and specific inhibition of hormone sensitive lipase. Abstracts for the 46th International Conference on the Bioscience of Lipids136(2005).
Room temperature
in continental US; may vary elsewhere
SMILES
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COc1nn(c2ccc(NC(=O)OCc3ccccc3)c(C)c2)c(=O)o1
Background Reading
Saltiel, A.R. Another hormone-sensitive triglyceride lipase in fat cells. Proc Natl Acad Sci USA97(2)535-537(2000 Jan 18).
Ali, Y.B., Müller, G., Petry, S., et al. Kinetic characterization and specific inhibition of hormone sensitive lipase. Abstracts for the 46th International Conference on the Bioscience of Lipids136(2005).
Kraemer, F.B., and Shen, W. Hormone-sensitive lipase: Control of intracellular tri-(di-)acylglycerol and cholesteryl ester hydrolysis. J Lipid Res431585-1594(2002 Jan 1).
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1 mg
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5 mg
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10 mg
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25 mg
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