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4β-hydroxy Cholesterol

Catalog No.GC10762

An endogenous marker for CYP3A4/5 activity

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4β-hydroxy Cholesterol Chemical Structure

Cas No.: 17320-10-4

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1mg
52,00 $
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5mg
108,00 $
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10mg
200,00 $
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25mg
398,00 $
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Sample solution is provided at 25 µL, 10mM.

Description of 4β-hydroxy Cholesterol

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.

Chemical Properties of 4β-hydroxy Cholesterol

Cas No. 17320-10-4 SDF
Chemical Name 5 cholesten-3β,4β-diol
Canonical SMILES O[C@H]([C@@H]1O)CC[C@@]2(C)C1=CC[C@]3([H])[C@]2([H])CC[C@@]4(C)[C@@]3([H])CC[C@]4([H])[C@H](C)CCCC(C)C
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
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of 4β-hydroxy Cholesterol

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1 mg 5 mg 10 mg
1 mM 2.4832 mL 12.4162 mL 24.8324 mL
5 mM 0.4966 mL 2.4832 mL 4.9665 mL
10 mM 0.2483 mL 1.2416 mL 2.4832 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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