Date published: 2026-1-11

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4α-Hydroxy Cholesterol (CAS 34310-86-6)

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Alternate Names:
(3β,4α)-Cholest-5-ene-3,4-diol; Cholest-5-ene-3β,4α-diol
Application:
4α-Hydroxy Cholesterol is a potential ligand for the nuclear receptor LXR and also a new endogenous CYP3A marker
CAS Number:
34310-86-6
Molecular Weight:
402.65
Molecular Formula:
C27H46O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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4α-Hydroxy Cholesterol (4HC) is a metabolite of Cholesterol. It is formed from Cholesterol by the drug-metabolizing enzyme cytochrome P 450 3A4. It is a potential ligand for the nuclear receptor LXR and a new endogenous CYP3A marker. 4α-Hydroxy Cholesterol is involved in regulation of cholesterol homeostasis, cell membrane fluidity, and cell signaling pathways. It has also been shown to have anti-inflammatory, anti-atherosclerotic, and anti-cancer effects.


4α-Hydroxy Cholesterol (CAS 34310-86-6) References

  1. 4beta-hydroxycholesterol as an endogenous marker for CYP3A4/5 activity. Stability and half-life of elimination after induction with rifampicin.  |  Diczfalusy, U., et al. 2009. Br J Clin Pharmacol. 67: 38-43. PMID: 19006545
  2. A validated liquid chromatography-tandem mass spectrometry method for the quantitative determination of 4β-hydroxycholesterol in human plasma.  |  van de Merbel, NC., et al. 2011. J Pharm Biomed Anal. 55: 1089-95. PMID: 21507593
  3. Quantification of 4-beta-hydroxycholesterol in human plasma using automated sample preparation and LC-ESI-MS/MS analysis.  |  Goodenough, AK., et al. 2011. Chem Res Toxicol. 24: 1575-85. PMID: 21728364
  4. Biological activities of the LXRα and β agonist, 4β-hydroxycholesterol, and of its isomer, 4α-hydroxycholesterol, on oligodendrocytes: effects on cell growth and viability, oxidative and inflammatory status.  |  Nury, T., et al. 2013. Biochimie. 95: 518-30. PMID: 23220593
  5. Improved synthesis and in vitro evaluation of the cytotoxic profile of oxysterols oxidized at C4 (4α- and 4β-hydroxycholesterol) and C7 (7-ketocholesterol, 7α- and 7β-hydroxycholesterol) on cells of the central nervous system.  |  Nury, T., et al. 2013. Eur J Med Chem. 70: 558-67. PMID: 24211631
  6. 4β-Hydroxycholesterol as an endogenous biomarker of CYP3A activity in cynomolgus monkeys.  |  Li, K., et al. 2014. Drug Metab Dispos. 42: 839-43. PMID: 24595680
  7. Quantitation of P450 3A4 endogenous biomarker - 4β-hydroxycholesterol - in human plasma using LC/ESI-MS/MS.  |  Huang, MQ., et al. 2014. Biomed Chromatogr. 28: 794-801. PMID: 24861746
  8. Evaluation of 4β-Hydroxycholesterol as a Clinical Biomarker of CYP3A4 Drug Interactions Using a Bayesian Mechanism-Based Pharmacometric Model.  |  Leil, TA., et al. 2014. CPT Pharmacometrics Syst Pharmacol. 3: e120. PMID: 24964282
  9. Cholesterol transformations during heat treatment.  |  Derewiaka, D. and Molińska née Sosińska, E. 2015. Food Chem. 171: 233-40. PMID: 25308664
  10. Recommendations on the Development of a Bioanalytical Assay for 4β-Hydroxycholesterol, an Emerging Endogenous Biomarker of CYP3A Activity.  |  Aubry, AF., et al. 2016. AAPS J. 18: 1056-1066. PMID: 27350147
  11. Mass spectrometry profiling of oxysterols in human sperm identifies 25-hydroxycholesterol as a marker of sperm function.  |  Zerbinati, C., et al. 2017. Redox Biol. 11: 111-117. PMID: 27912195
  12. Evaluation of 4β-Hydroxycholesterol and 25-Hydroxycholesterol as Endogenous Biomarkers of CYP3A4: Study with CYP3A-Humanized Mice.  |  Nitta, SI., et al. 2018. AAPS J. 20: 61. PMID: 29858698
  13. Quantitative analysis of 4β- and 4α‑hydroxycholesterol in human plasma and serum by UHPLC/ESI-HR-MS.  |  Hautajärvi, H., et al. 2018. J Chromatogr B Analyt Technol Biomed Life Sci. 1100-1101: 179-186. PMID: 30340067
  14. 4β-Hydroxycholesterol Signals From the Liver to Regulate Peripheral Cholesterol Transporters.  |  Salonurmi, T., et al. 2020. Front Pharmacol. 11: 361. PMID: 32292343
  15. Sensitive UHPLC-MS/MS quantification method for 4β- and 4α-hydroxycholesterol in plasma for accurate CYP3A phenotyping.  |  Suzuki, Y., et al. 2022. J Lipid Res. 63: 100184. PMID: 35181316

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

4α-Hydroxy Cholesterol, 1 mg

sc-363858
1 mg
$520.00

4α-Hydroxy Cholesterol, 2 mg

sc-363858A
2 mg
$921.00

4α-Hydroxy Cholesterol, 5 mg

sc-363858B
5 mg
$1727.00