89355  22(R)-hydroxy Cholesterol

22(α)-hydroxy Cholesterol (CAS 17954-98-2)

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• See more Nuclear Receptors; Steroids; Atherosclerosis; Oxidative Injury

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The liver X receptors (LXRα and LXRβ) are nuclear hormone receptors whose native ligands are oxysterols.1 22(R)-hydroxy Cholesterol (22(R)-OH-Ch) is an endogenous agonist for the LXRs. The EC50 value for ligand-dependent activation of LXRα by 22(R)-OH-Ch is approximately 325 nM.2 The LXRs regulate the oxysterol-induced expression of cholesterol 7α-hydroxylase, the rate limiting enzyme of classic bile acid synthesis. 22(R)-OH-Ch, acting through LXR in concert with the retinoid X receptor (RXR), its heterodimerization partner, induces the expression of the ABCA1 reverse cholesterol transporter.3 This acts to increase the efflux of cholesterol from enterocytes and thus inhibit the overall absorption of cholesterol. 22(R)-OH-Ch can be used as an endogenous positive control for the testing of LXR agonists, which have potential as therapeutic agents for the treatment of atherosclerosis.
1  Repa, J.J., Turley, S.D., Lobaccaro, J.A., et al. Regulation of absorption and ABC1-mediated efflux of cholesterol by RXR heterodimers. Science 289 1524-1529 (2000).
2  Spencer, T.A., Dansu, L., Russel, J.S., et al. Pharmacophore analysis of the nuclear oxysterol receptor LXRα J Med Chem 44, 886-897 (2001).
3  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 28240-28245 (2000).


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Warning This product is not for human or veterinary use.

Pricing updated 2010-03-18.
Prices are subject to change without notice.

Stability of this item is suitable for room temperature overnight shipping. If shipment on ice is desired, it must be requested when the order is placed.

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