4β-hydroxy Cholesterol

4β-hydroxy Cholesterol

Catalog Number:
FC01366522APE
Mfr. No.:
APE-C5540
Price:
$236
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          Background

          4β-hydroxy Cholesterol is an endogenous marker for CYP3A4/5 activity [1]. Cytochome P450 3A4 (CYP3A4) and CYP3A5 are important drug-metabolizing enzymes that oxidize small foreign organic molecules, such as toxins or drugs, and remove them from the body. They exhibit a large variation in hepatic expression and biological activity between different individuals. Patients treated with drugs known to be strong inducers of CYP3A4/5 have highly elevated levels of 4β-hydroxycholesterol in the circulation [1]. 4β-hydroxy Cholesterol, an endogenous oxysterol found in human circulation, is formed from cholesterol by cytochrome P450 (CYP) 3A4 and CYP3A5. In 12 different occasions during a 3-month period, The CVs for 4β-hydroxycholesterol ranged from 4.8 to 13.2% with an average CV of 7.1% at an average concentration of 30.8 ng/ml. In 24 volunteers treated with rifampicin, a strong CYP3A4/5 inducer, 4β-hydroxycholesterol increased in a dose-dependent way, while the isomer 4α-hydroycholesterol was not influenced by rifampicin treatment. These results suggested that 4β-hydroxy Cholesterol is an endogenous marker for CYP3A4/5 activity [1].

          Reference:[1]. Diczfalusy U, Kanebratt KP, Bredberg E, et al. 4beta-hydroxycholesterol as an endogenous marker for CYP3A4/5 activity. Stability and half-life of elimination after induction with rifampicin. Br J Clin Pharmacol. 2009 Jan;67(1):38-43.

      • Properties
        • Categories
          marker for CYP3A4/5 activity
          Alternative Name
          5 cholesten-3β,4β-diol
          CAS Number
          17320-10-4
          Molecular Formula
          C27H46O2
          Molecular Weight
          402.7
          Appearance
          A crystalline solid
          Solubility
          ≤20mg/ml in ethanol;0.1mg/ml in DMSO;2mg/ml in dimethyl formamide
          Storage
          Store at -20°C
          SMILES
          O[[email protected]]([[email protected]@H]1O)CC[[email protected]@]2(C)C1=CC[[email protected]]3([H])[[email protected]]2([H])CC[[email protected]@]4(C)[[email protected]@]3([H])CC[[email protected]]4([H])[[email protected]](C)CCCC(C)C

          * For Research Use Only

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