4β-hydroxy Cholesterol |
Catalog No.GC10762 |
An endogenous marker for CYP3A4/5 activity
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 17320-10-4
Sample solution is provided at 25 µL, 10mM.
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.
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. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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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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Calculation results:
Working concentration: mg/ml;
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.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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