Réactifs et instruments pour l'immunologie, la biologie cellulaire et la biologie moléculaire.
 
> FICZ [172922-91-7]

FICZ [172922-91-7]

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Référence HY-12451-1mg

Conditionnement : 1mg

Marque : MedChemExpress

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Description

FICZ is a potent aryl hydrocarbon receptor (AhR) agonist with a Kd of 70 pM.

Cellular Effect
Cell Line Type Value Description References
HepG2 EC50
2.04 nM
Compound: 2; FICZ
Agonist activity at AhR in human HepG2 cells assessed as induction of CYP1A1 expression after 24 hrs by ethoxyresorufin-O-deethylase assay
Agonist activity at AhR in human HepG2 cells assessed as induction of CYP1A1 expression after 24 hrs by ethoxyresorufin-O-deethylase assay
[PMID: 31952965]
In Vitro

FICZ (0.01 nM-1 µM) alone or in combination with 50 nM MNF induces sustained CYP1A1 activity and leads to oxidative stress and activation of apoptosis via a mitochondrial-dependent pathway. In HepG2 cells, FICZ stimulates cell growth at low concentrations but inhibits cell growth at high concentrations[1]. FICZ (10,000-30,000 nM) significantly decreases CEH viability with an estimated LC50 (95% confidence intervals) of 14,000 nM. FICZ shows concentration-dependent effects on EROD activity in CEH cultures, with the mean EC50 values at 3, 8, and 24 h of 0.016 nM, 0.80 nM, and 11 nM, respectively[2]. FICZ treatment increases transcript expression of CYP1A1 in a dose-dependent manner in both the parental iPSC line and the CYP1A1 targeted clone[3]. CYP1 inhibition in the presence of FICZ results in enhanced AHR activation, suggesting that FICZ accumulates in the cell when its metabolism is blocked. CYP1 enzymes plays a role in regulating biological effects of FICZ[4].
Nuclear export and degradation of the AHR protein are two additional steps in the AHR-mediated signal transduction pathway[5].
Exposure to AhR agonists causes AhR-expressing cells to downregulate the receptor through the ubiquitin/proteasome degradation pathway[6].

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

FICZ Related Antibodies

Solvant et solubilité
In Vitro: 

DMSO : 10 mg/mL (35.17 mM; Need ultrasonic and warming; 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 3.5173 mL 17.5864 mL 35.1729 mL
5 mM 0.7035 mL 3.5173 mL 7.0346 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: 1.11 mg/mL (3.90 mM); Suspended solution; Need ultrasonic

  • Protocol 2

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

    Solubility: ≥ 0.83 mg/mL (2.92 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.83 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 (8.3 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  15% Solutol HS 15    10% Cremophor EL    35% PEG400    40% Water

    Solubility: 3.33 mg/mL (11.71 mM); Suspended solution; Need ultrasonic
Pureté et documentation
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