25-Hydroxycholesterol [2140-46-7]

Referência HY-113134-5mg

Tamanho : 5mg

Marca : MedChemExpress


Description

25-Hydroxycholesterol (25-OHC) is a metabolite of cholesterol that is produced and secreted by macrophages in response to Toll-like receptor (TLR) activation. 25-hydroxycholesterol is a potent (EC50≈65 nM) and selective suppressor of IgA production by B cells.

IC50 & Target

Human Endogenous Metabolite

 

Cellular Effect
Cell Line Type Value Description References
CHO-K1 IC50
0.3 μM
Compound: 25-hydroxycholesterol
Inhibition of SREBP2 activation expressed in CHO-K1 cells co-transfected with pSRE-Luc plasmid assessed as inhibition of luciferase expression after 20 hrs by luciferase reporter gene assay
Inhibition of SREBP2 activation expressed in CHO-K1 cells co-transfected with pSRE-Luc plasmid assessed as inhibition of luciferase expression after 20 hrs by luciferase reporter gene assay
[PMID: 21561152]
HEK293 EC50
2.3 μM
Compound: 11, 25-HC
Binding affinity to human GFP-tagged NPC1L1 L1072T/L1168I mutant expressed in HEK293 cells assessed as localization to endoplasmic reticulum and plasma membrane after 24 hrs by fluorescence microscopic analysis
Binding affinity to human GFP-tagged NPC1L1 L1072T/L1168I mutant expressed in HEK293 cells assessed as localization to endoplasmic reticulum and plasma membrane after 24 hrs by fluorescence microscopic analysis
[PMID: 23830695]
HEK293 EC50
3.3 μM
Compound: 1, 25HC
Binding affinity to FLAG/tGFP-tagged NPC1 I1061T mutant (unknown origin) expressed in HEK293 cells assessed as localization after 24 hrs by fluorescence microscopy
Binding affinity to FLAG/tGFP-tagged NPC1 I1061T mutant (unknown origin) expressed in HEK293 cells assessed as localization after 24 hrs by fluorescence microscopy
[PMID: 24928400]
HEK293 EC50
>10000 nM
Compound: 39
Positive allosteric modulation of recombinant human GluN1/GluN2B receptor stably expressed in HEK293 cells assessed as increase in glycine/L-glutamate-induced channel current at -70 mV holding potential by IonWork two-electrode voltage clamp method
Positive allosteric modulation of recombinant human GluN1/GluN2B receptor stably expressed in HEK293 cells assessed as increase in glycine/L-glutamate-induced channel current at -70 mV holding potential by IonWork two-electrode voltage clamp method
[PMID: 31390523]
HEK293 EC50
>10000 nM
Compound: 39
Positive allosteric modulation of recombinant human GluN1/GluN2A receptor stably expressed in HEK293 cells assessed as increase in glycine/L-glutamate-induced channel current at -70 mV holding potential by IonWork two-electrode voltage clamp method
Positive allosteric modulation of recombinant human GluN1/GluN2A receptor stably expressed in HEK293 cells assessed as increase in glycine/L-glutamate-induced channel current at -70 mV holding potential by IonWork two-electrode voltage clamp method
[PMID: 31390523]
HEK293 EC50
0.63 μM
Compound: 25HC
Induction of human HMGCR-dCat-ELuc degradation expressed in HEK293 cells assessed as reduction in luciferase activity after 4 hrs by luciferase reporter assay
Induction of human HMGCR-dCat-ELuc degradation expressed in HEK293 cells assessed as reduction in luciferase activity after 4 hrs by luciferase reporter assay
[PMID: 31902650]
HepG2 IC50
0.3 μM
Compound: 25-hydroxy-cholesterol
Tested for its inhibitory activity against HMG-CoA reductase transcription in HepG2 cells
Tested for its inhibitory activity against HMG-CoA reductase transcription in HepG2 cells
[PMID: 8057282]
Vero IC50
>128 μM
Compound: 7
Cytotoxicity against african green monkey Vero cells by tetrazolium dye reduction assay
Cytotoxicity against african green monkey Vero cells by tetrazolium dye reduction assay
[PMID: 24084159]
In Vitro

The synthesis of 25-hydroxycholesterol is catalyzed by the enzyme cholesterol 25-hydroxylase, which uses cholesterol and molecular oxygen as substrates and NADPH as a cofactor. 25-hydroxycholesterol is a potent bioactive lipid in the innate and adaptive immune systems[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvant et solubilité
In Vitro: 

Ethanol : 14.29 mg/mL (35.49 mM; Need ultrasonic)

DMSO : 5 mg/mL (12.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4835 mL 12.4177 mL 24.8355 mL
5 mM 0.4967 mL 2.4835 mL 4.9671 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 0.5 mg/mL (1.24 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 0.5 mg/mL (1.24 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Pureté et documentation
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