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 hormone sensitive lipase exhibiting an IC₅₀ of 90 nM for the recombinant enzyme.³ The in vivo pharmacological efficacy of CAY10499 has not been reported.

≥98%

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1.Saltiel, A.R. Another hormone-sensitive triglyceride lipase in fat cells. Proceedings of the National Academy of Sciences of the United States of America 97(2), 535-537 (2000).

2.Kraemer, F.B. and Shen, W.J. Hormone-sensitive lipase: Control of intracellular tri-(di-)acylglycerol and cholesteryl ester hydrolysis. Journal of Lipid Research 43, 1585-1594 (2002).

3.Ali, Y.B.,Müller, G.,Petry, S., et al. Kinetic characterization and specific inhibition of hormone sensitive lipase. 136,.