| 22(R)-hydroxy Cholesterolendogenous agonist for LXRs |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
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Chemical structure
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| Cas No. | 17954-98-2 | SDF | Download SDF |
| Synonyms | Narthesterol | ||
| Chemical Name | cholest-5-ene-3β,22R-diol | ||
| Canonical SMILES | CC(C)CC[C@@H](O)[C@@H](C)C1CCC2C3CC=C4C[C@@H](O)CC[C@]4(C)C3CC[C@@]21C | ||
| Formula | C27H46O2 | M.Wt | 402.7 |
| Solubility | ≤20mg/ml in ethanol;0.1mg/ml in DMSO;2mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
EC50: 325 nM
22(R)-hydroxy cholesterol is an endogenous agonist for liver X receptors (LXRs).
The liver X receptors, LXRR and LXRα, together with the farnesoid X receptor, FXR, form a subfamily of these orphan receptors. Recently, it has been reported that LXR and FXR are hormone receptors for oxysterols and bile acids, respectively.
In vitro: Previous study found that 22(R)-hydroxycholesterol was only found in the adrenals as an intermediate in pregnenolone biosynthesis, not similar with 24(R), 25-epoxycholesterol and 20(S)-hydroxycholesterol. In addition, the hydroxyl groups of 22(R)-hydroxycholesterol as well as its analogs of 23(S)-hydroxycholesterol and 24(S)-hydroxycholesterol would all lie between 2.0-2.5 from Trp443 [1]. In another study, the ABC1 mRNA expression could be induced in an additive fashion by 22(R)-hydroxycholesterol and 9-cis-retinoic acid in cultured macrophages, indicating induction by nuclear hormone receptors of the liver X receptor and retinoid X receptor family. Moreover, the upstream promoter was induced 7-fold by the treatment of 22(R)-hydroxycholesterol when transfected into RAW macrophages [2].
In vivo: So far, there is no animal in vivo data reported.
Clinical trial: Up to now, 22(R)-hydroxy cholesterol is still in the preclinical development stage.
References:[1] T. A. Spencer, L. Dansu, J. S. Russel, et al. Pharmacophore analysis of the nuclear oxysterol receptor LXRα. Journal of Medicinal Chemistry 44, 886-897(2001).[2] Costet P, Luo Y, Wang N, Tall AR. Sterol-dependent transactivation of the ABC1 promoter by the liver X receptor/retinoid X receptor. J Biol Chem. 2000 Sep 8;275(36):28240-5.
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