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> CH-223191 [301326-22-7]

CH-223191 [301326-22-7]

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Katalog-Nummer HY-12684-5mg

Size : 5mg

Marke : MedChemExpress

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CH-223191 is a potent and specific antagonist of aryl hydrocarbon receptor (AhR). CH-223191 inhibits TCDD-mediated nuclear translocation and DNA binding of AhR, and inhibits TCDD-induced luciferase activity with an IC50 of 0.03 μM.

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CH-223191 Chemische Struktur

CH-223191 Chemische Struktur

CAS. Nr. : 301326-22-7

This product is a controlled substance and not for sale in your territory.

Based on 69 publication(s) in Google Scholar

    CH-223191 purchased from MedChemExpress. Usage Cited in: Nat Metab. 2023 Feb 13.  [Abstract]

    CH223191 suppresses GSK3β and Akt phosphorylation in chow-fed mice.

    CH-223191 purchased from MedChemExpress. Usage Cited in: Chemosphere. 2018 Oct 23;216:372-378.  [Abstract]

    AhR mediates EOM-inhibited cardiac differentiation by downregulating β-catenin expression in P19 cells. mRNA expression changes of β-catenin by Q-PCR. The concentrations of CH (CH223191, AhR antagonist) and CHIR (CHIR99021, Wnt activator) are 0.25 and 0.5 μM respectively.

    CH-223191 purchased from MedChemExpress. Usage Cited in: Chemosphere. 2018 Oct 23;216:372-378.  [Abstract]

    AhR mediates EOM-inhibited cardiac differentiation by downregulating β-catenin expression in P19 cells. Percentage of cTnT positive cells at differentiation day 14. The concentrations of CH (CH223191, AhR antagonist) and CHIR (CHIR99021, Wnt activator) are 0.25 and 0.5 μM respectively.

    CH-223191 purchased from MedChemExpress. Usage Cited in: Chemosphere. 2018 Oct 23;216:372-378.  [Abstract]

    AhR mediates EOM-inhibited cardiac differentiation by downregulating β-catenin expression in P19 cells. Percentage of cTnT positive cells at differentiation day 14. The concentrations of CH (CH223191, AhR antagonist) and CHIR (CHIR99021, Wnt activator) are 0.25 and 0.5 μM respectively.

    CH-223191 purchased from MedChemExpress. Usage Cited in: Chemosphere. 2018 Oct 23;216:372-378.  [Abstract]

    Proliferation of P19 cells exposed to EOM in the presence or absence of CH. Represent images of EdU staining (red) and the quantification results.

    CH-223191 purchased from MedChemExpress. Usage Cited in: Toxicology. 2016 May 20;355-356:31-38.  [Abstract]

    Western analysis of β-catenin protein level in zebrafish embryos exposed to EOM in the presence or absence of CH/CHIR (n = 3). Different letters indicate significant differences. Moreover, both CH and CHIR attenuate the EOM-induced changes in the protein level of b-catenin and in EROD activity.
    Beschreibung

    CH-223191 is a potent and specific antagonist of aryl hydrocarbon receptor (AhR). CH-223191 inhibits TCDD-mediated nuclear translocation and DNA binding of AhR, and inhibits TCDD-induced luciferase activity with an IC50 of 0.03 μM[1].

    In Vitro

    CH-223191 (0.1-10 μM; pre-treated 1 hour) inhibits TCDD-caused cytochrome P450 1A1 mRNA expression in a in dose-dependent manner[1].
    CH-223191 (0.1-10 μM; pre-treated 1 hour) causes a concentration-dependent inhibition of TCDD-induced cytochrome P450 enzyme activity[1].

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

    CH-223191 Related Antibodies

    RT-PCR[1]

    Cell Line: HepG2 cells
    Concentration: 0.1-10 μM
    Incubation Time: 1 hour
    Result: Caused inhibition of TCDD-induced cytochrome P450 mRNA expression.

    Western Blot Analysis[1]

    Cell Line: HepG2 cells
    Concentration: 0.1-10 μM
    Incubation Time: 1 hour
    Result: Decreased TCDD-caused cytochrome P450 1A1 protein Treatment.
    In Vivo

    CH-223191 (10 mg/kg; once a day; 25 days) suppresses cytochrome P450 1A1 expression and the intrahepatocyte fat content in liver, reduces activity of AST and ALT in TCDD-treated mice[1].

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

    Animal Model: Male ICR mice (6 weeks old)[1]
    Dosage: 10 mg/kg
    Administration: 10 mg/kg; once a day; 25 days
    Result: Prevented TCDD-elicited cytochrome P450 induction, liver toxicity, and wasting syndrome in mice.
    Molekulargewicht

    333.39

    Formel

    C19H19N5O
    CAS. Nr.

    301326-22-7
    Appearance

    Solid

    Color

    Yellow to orange

    SMILES

    O=C(C1=CC=NN1C)NC2=CC=C(/N=N/C3=CC=CC=C3C)C=C2C
    Versand

    Room temperature in continental US; may vary elsewhere.
    Speicherung
    Powder -20°C 3 years
    4°C 2 years

    *The compound is unstable in solutions, freshly prepared is recommended.

    Lösungsmittel & Löslichkeit
    In Vitro: 

    DMSO : 100 mg/mL (299.95 mM; ultrasonic and warming and heat to 60°C; 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 2.9995 mL 14.9974 mL 29.9949 mL
    5 mM 0.5999 mL 2.9995 mL 5.9990 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    • Molaritätsrechner

    • Verdünnungsrechner

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 0.33 mg/mL (0.99 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.33 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (3.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

    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:  50% PEG300    50% Saline

      Solubility: 20 mg/mL (59.99 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *The compound is unstable in solutions, freshly prepared is recommended.

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Reinheit & Dokumentation

    Purity: 99.96%

    COA (247 KB) HNMR (269 KB) RP-HPLC (242 KB) LCMS (93 KB)

    Handling Instructions (2659 KB)
    Verweise

    • [1]. Kim SH, et al. Novel compound 2-methyl-2H-pyrazole-3-carboxylic acid (2-methyl-4-o-tolylazo-phenyl)-amide (CH-223191) prevents 2,3,7,8-TCDD-induced toxicity by antagonizing the aryl hydrocarbon receptor. Mol Pharmacol. 2006 Jun;69(6):1871-8. Epub 2006 Mar 15.  [Content Brief]

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.9995 mL 14.9974 mL 29.9949 mL 74.9872 mL
    5 mM 0.5999 mL 2.9995 mL 5.9990 mL 14.9974 mL
    10 mM 0.2999 mL 1.4997 mL 2.9995 mL 7.4987 mL
    15 mM 0.2000 mL 0.9998 mL 1.9997 mL 4.9991 mL
    20 mM 0.1500 mL 0.7499 mL 1.4997 mL 3.7494 mL
    25 mM 0.1200 mL 0.5999 mL 1.1998 mL 2.9995 mL
    30 mM 0.1000 mL 0.4999 mL 0.9998 mL 2.4996 mL
    40 mM 0.0750 mL 0.3749 mL 0.7499 mL 1.8747 mL
    50 mM 0.0600 mL 0.2999 mL 0.5999 mL 1.4997 mL
    60 mM 0.0500 mL 0.2500 mL 0.4999 mL 1.2498 mL
    80 mM 0.0375 mL 0.1875 mL 0.3749 mL 0.9373 mL
    100 mM 0.0300 mL 0.1500 mL 0.2999 mL 0.7499 mL
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    CH-223191 Related Classifications

    Help & FAQs

    Keywords:

    CH-223191301326-22-7CH223191CH 223191Aryl Hydrocarbon ReceptorAhRInhibitorinhibitorinhibit

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