DMHCA

DMHCA is a liver X receptor (LXR) agonist.¹ It activates LXRα and LXRβ in CV-1 cells expressing the human receptors in reporter assays (EC₅₀ = 2 µM for both). DMHCA also inhibits ∆²⁴-dehydrocholesterol reductase (DHCR24; IC₅₀ = 0.7 nM).² It does not induce steatosis or increase liver triglyceride levels compared with the LXR agonist T0901317 (Item No. 71810) in mice when administered at a dose of 80 mg/kg.³ DMHCA (8 mg/kg) reduces the size of atherosclerotic lesions in ApoE^-/- mice fed a Western diet. It decreases proteinuria and hepatic cholesterol levels in a mouse model of diabetic nephropathy induced by streptozotocin (Item No. 13104).⁴

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1. Janowski, B.A., Grogan, M.J., Jones, S.A., et al. Structural requirements of ligands for the oxysterol liver X receptors LXRα and LXRβ. Proc. Natl. Acad. Sci. USA 96(1), 266-271 (1999).

2. Müller, C., Hemmers, S., Bartl, N., et al. New chemotype of selective and potent inhibitors of human delta 24-dehydrocholesterol reductase. Eur. J. Med. Chem. 140, 305-320 (2017).

3. Kratzer, A., Buchebner, M., Pfeifer, T., et al. Synthetic LXR agonist attenuates plaque formation in apoE-/- mice without inducing liver steatosis and hypertriglyceridemia. J. Lipid. Res. 50(2), 312-326 (2009).

4. Patel, M., Wang, X.X., Magomedova, L., et al. Liver X receptors preserve renal glomerular integrity under normoglycaemia and in diabetes in mice. Diabetologia 57(2), 435-436 (2014).