344327-48-6

The liver X receptors (LXRα and LXRβ) are nuclear hormone receptors whose native ligands are oxysterols.¹ Acetyl podocarpic acid anhydride (APD) is a potent, semisynthetic LXR agonist derived from extracts of the mayapple. APD acting through LXR in concert with the retinoid X receptor (RXR), its heterodimerization partner, induces the expression of the ABCA1 reverse cholesterol transporter.² This acts to increase the efflux of cholesterol from enterocytes and thus inhibits the overall absorption of cholesterol (ED₅₀ value of 1 nM).³ In transient transactivation assays, APD was found to be approximately 1,000 times more potent and have 8-10-fold greater maximal stimulation of LXR than 22(R)-hydroxy cholesterol.^3,4 APD can be used as a positive control for the testing of LXR agonists, which have potential as therapeutic agents for the treatment of atherosclerosis.

ChEBI:Acetyl Podocarpic Acid Anhydride is a diterpenoid.

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1. Repa, J.J., Turley, S.D., Lobaccaro, J.M.A., et al. Regulation of absorption and ABC1-mediated efflux of cholesterol by RXR heterodimers Science 289(5484),1524-1529(2000).
2. Costet, P., Luo, Y., Wang, N., et al. Sterol-dependent transactivation of the ABC1 promoter by the liver X receptor/retinoid X receptor J. Biol. Chem. 275(36),28240-28245(2000).
3. Sparrow, C.P., Baffic, J., Lam, M.H., et al. A potent synthetic LXR agonist is more effective than cholesterol loading at inducing ABCA1 mRNA and stimulating cholesterol efflux J. Biol. Chem. 277(12),10021-10027(2002).
4. Singh, S.B., Ondeyka, J.G., Liu, W., et al. Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters Bioorg. Med. Chem. Lett. 15(11),2824-2828(2005).