الصفحة الرئيسية>>Signaling Pathways>> Immunology/Inflammation>> Aryl Hydrocarbon Receptor>>FICZ

FICZ (Synonyms: FICZ)

رقم الكتالوجGC36043

FICZ هو ناهض قوي لمستقبلات أريل الهيدروكربونية (AhR) مع Kd 70 pM

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FICZ التركيب الكيميائي

Cas No.: 172922-91-7

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
363٫00
متوفر
1mg
116٫00
متوفر
5mg
441٫00
متوفر
10mg
603٫00
متوفر
25mg
1112٫00
متوفر
50mg
1715٫00
متوفر

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    GlpBio Citations
  • Bioactive Compounds Premium Provider

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

BMSCs

Preparation Method

To detect the inflammatory responses of BMSCs, the cells were rendered quiescent by serum starvation and then stimulated with 1 µg ml-1 lipopolysaccharide (LPS) supplemented with 500 nM FICZ, 1 µM SR1 (AhR antagonist StemRegenin 1) or dimethyl sulphoxide (DMSO) for 6 h.

Reaction Conditions

500 nM; 6h

Applications

The results demonstrated that LPS significantly up-regulated the expressions of IL-1β, 6 and TNF-α and FICZ or SR1 prevented or exacerbated the inflammatory responses.

Animal experiment [2]:

Animal models

Male C57BL/6J mice (24-29 g, 10 weeks of age)

Preparation Method

Animals were randomized into the following four groups: Sham-treated with vehicle or with FICZ and TAC-treated with vehicle or with FICZ. Treatment with FICZ (i.p., 5 mg kg-1) or with vehicle (dimethylsulfoxide) was initiated 5 min after Sham or TAC surgery and was repeated 2 days after surgery. CMRI was performed on 8 animals in each group before and 3 days after surgery. Subsequently, animals were anesthetized with isoflurane, and hearts were excised, weighed, and prepared for biochemical and immunofluorescence studies.

Dosage form

5 mg/kg; i.p.,

Applications

Cardiac structure and function were evaluated by cardiac magnetic resonance imaging (CMRI) before and 3 days after Sham or TAC surgery in mice treated with FICZ or with vehicle, and cardiac tissue was used for biochemical studies. CMRI analysis revealed that FICZ improved cardiac function and attenuated cardiac hypertrophy.

References:

Huang J, et al. Beneficial roles of the AhR ligand FICZ on the regenerative potentials of BMSCs and primed cartilage templates. RSC Adv. 2022 Apr 13;12(18):11505-11516.
Tamayo M, et al. The Aryl Hydrocarbon Receptor Ligand FICZ Improves Left Ventricular Remodeling and Cardiac Function at the Onset of Pressure Overload-Induced Heart Failure in Mice. Int J Mol Sci. 2022 May 12;23(10):5403.

Background

FICZ (Formyl-indolo [3,2-b] carbazole), as an endogenous ligand for the aryl hydrocarbon receptor (AhR), can exert pleiotropic effects including protection against inflammation, fibrosis, and oxidative stress[1].

In vitro, treatment with 0.01 nM-1 µM FICZ in HepG2 cells, FICZ stimulated cell growth at low concentrations but inhibited cell growth at high concentrations[2]. In vitro experiment it demonstrated that treatment LPS combined with 200 nM FICZ in YAMC cells did not influence LPS-induced IL-6 release[3]. In vitro, 50 µM FICZ obviously induced apoptosis, whereas all tested compounds in higher concentrations (L-KYN 1 mM, KYNA 5 mM, FICZ 50 µM) increased necrosis in melanoma A375 cells. Statistically, FICZ obviously inhibited DNA synthesis in A375 cells at a concentration range of 10-6-50 µM, but there is only observed inhibitory effect on RPMI7951 cells in the highest tested micromolar concentrations[4].

In vivo efficacy test it shown that per mouse was treatment with 1 µg (50 µg/kg) intraperitoneally enhanced the level of IL-22 in colonic samples, and ameliorated colitis induced by TNBS (trinitrobenzene sulfonic acid) or DSS (dextran sulfate sodium)[5]. In vivo, 10 µg/kg FICZ in mice orally resulted in transient AhR activation, with the effect waning in less than 18h[6].

[1]Tamayo M, et al. The Aryl Hydrocarbon Receptor Ligand FICZ Improves Left Ventricular Remodeling and Cardiac Function at the Onset of Pressure Overload-Induced Heart Failure in Mice. Int J Mol Sci. 2022 May 12;23(10):5403.

[2]Mohammadi-Bardbori A, et al. The highly bioactive molecule and signal substance 6-formylindolo[3,2-b]carbazole (FICZ) plays bi-functional roles in cell growth and apoptosis in vitro. Arch Toxicol. 2017 Oct;91(10):3365-3372.

[3]Li X, et al. 6-Formylindolo (3, 2-b) Carbazole (FICZ)-mediated protection of gut barrier is dependent on T cells in a mouse model of alcohol combined with burn injury. Biochim Biophys Acta Mol Basis Dis. 2020 Nov 1;1866(11):165901.

[4]Walczak K, et al. Effect of Tryptophan-Derived AhR Ligands, Kynurenine, Kynurenic Acid and FICZ, on Proliferation, Cell Cycle Regulation and Cell Death of Melanoma Cells-In Vitro Studies. Int J Mol Sci. 2020 Oct 26;21(21):7946.

[5]Rannug A. How the AHR Became Important in Intestinal Homeostasis-A Diurnal FICZ/AHR/CYP1A1 Feedback Controls Both Immunity and Immunopathology. Int J Mol Sci. 2020 Aug 8;21(16):5681.

[6]Wheeler JL, et al. Differential consequences of two distinct AhR ligands on innate and adaptive immune responses to influenza A virus. Toxicol Sci. 2014 Feb;137(2):324-34.

Chemical Properties

Cas No. 172922-91-7 SDF
المرادفات FICZ
Canonical SMILES O=CC1=C2C(NC3=C2C=CC=C3)=CC4=C1NC5=C4C=CC=C5
Formula C19H12N2O M.Wt 284.31
الذوبان DMSO : 10 mg/mL (35.17 mM) 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

Prepare stock solution
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
10 mM 0.3517 mL 1.7586 mL 3.5173 mL
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