1. Immunology/Inflammation
  2. Aryl Hydrocarbon Receptor
  3. Stemregenin 1

Stemregenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with IC50 of 127 nM.

For research use only. We do not sell to patients.

CAS No. : 1227633-49-9

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Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of Stemregenin 1:

Top Publications Citing Use of Products

    Stemregenin 1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jun 8;15(1):4909.  [Abstract]

    Stemregenin 1 (S: SR1; 1 μM; 3 days). WB of GLUT1 and GLUT3 expression in WCL and MEM fraction.

    Stemregenin 1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jun 8;15(1):4909.  [Abstract]

    Stemregenin 1 (S: SR1; 1 μM; 3 days). Operetta high content imaging analysis of 2-NBDG fluorescent tracer uptake.

    Stemregenin 1 purchased from MedChemExpress. Usage Cited in: RSC Adv. 2022 Apr 13;12(18):11505-11516.  [Abstract]

    Stemregenin 1 (SR1; 1 μM; 0-5 days).The absorbance at 450 nm of the CCK8 assay of the BMSCs. The number of viable BMSCs increased in all groups and there were no significant differences among the three groups on days 0, 1, 3 and 5 (p < 0.05).

    Stemregenin 1 purchased from MedChemExpress. Usage Cited in: RSC Adv. 2022 Apr 13;12(18):11505-11516.  [Abstract]

    Stemregenin 1 (SR1; 1 μM; 0-5 days).RT-PCR demonstrated that FICZ or SR1 prevented or exacerbated LPS-induced IL-1β, 6 and TNF-α, respectively.

    Stemregenin 1 purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Aug 11;11(18):8797-8812.

    N2a cells were treated with Dio (80 μM) with or without SR1 (2 μM) for 12 h. Whole cell lysates were collected and the NEP levels were determined.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Stemregenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with IC50 of 127 nM.

    IC50 & Target

    IC50: 127 nM (AhR)[1]

    In Vitro

    Stemregenin 1 (SR1) acts by antagonizing the aryl hydrocarbon receptor (AhR). Stemregenin 1 increases the number of CD34+ cells after 5 to 7 days with an EC50 of ~120 nM. Stemregenin 1 inhibits photoaffinity ligand (PAL) binding (IC50=40 nM) These results support the conclusion that Stemregenin 1 -induced CD34+ cell expansion is mediated through direct binding and inhibition of the AhR[1]. An aryl hydrocarbon receptor antagonist, Stemregenin 1 (SR1), robustly promotes ex vivo expansion of human CD34+ cells. Stemregenin 1 treatment accelerates the proliferation of CD34+ cells and decreases the expression levels of VentX[2].

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

    Clinical Trial
    Molecular Weight

    429.54

    Formula

    C24H23N5OS

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC(C)N1C2=NC(C3=CSC4=C3C=CC=C4)=NC(NCCC5=CC=C(O)C=C5)=C2N=C1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 62.5 mg/mL (145.50 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 2.3281 mL 11.6404 mL 23.2807 mL
    5 mM 0.4656 mL 2.3281 mL 4.6561 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    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: ≥ 2.5 mg/mL (5.82 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    • Protocol 2

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

      Solubility: 2.5 mg/mL (5.82 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    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 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.
    Purity & Documentation

    Purity: 99.95%

    References
    Cell Assay
    [1]

    A quantity of 250,000 CB-derived CD34+ cells are cultured with control conditions (DMSO, 0.01%) or StemRegenin 1 (0.75 μM) for 3 weeks. At this point control cultures had expanded 1080-fold and StemRegenin 1 treated cells expanded 2024-fold relative to starting cell numbers. A quantity of 30 to 30,000 uncultured CD34+ CB-derived cells or a fraction of the final culture equivalent to 30 to 10,000 starting cells are transplanted. The cells are injected intravenously via the retro-orbital route into sub-lethally irradiated (300 rads, 200 rads) 6- to 10-week-old NSG mice. Engraftment is performed within 24 h after irradiation. Engraftment is monitored by flow cytometric analysis of blood obtained via retro-orbital sinus or bone marrow using anti-human CD45 and anti-mouse CD45 antibodies. The mice are sacrificed between 13-16 weeks posttransplantation; bone marrow (from both femurs and tibiae), spleen and thymus are collected for analysis. For secondary engraftment, 50% of the bone marrow from each recipient mouse is transplanted into one secondary sub-lethally irradiated NSG mouse. Fifteen weeks after transplantation, bone marrow is harvested from the secondary mice and analyzed by flow cytometry[1].

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

    References

    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.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3281 mL 11.6404 mL 23.2807 mL 58.2018 mL
    5 mM 0.4656 mL 2.3281 mL 4.6561 mL 11.6404 mL
    10 mM 0.2328 mL 1.1640 mL 2.3281 mL 5.8202 mL
    15 mM 0.1552 mL 0.7760 mL 1.5520 mL 3.8801 mL
    20 mM 0.1164 mL 0.5820 mL 1.1640 mL 2.9101 mL
    25 mM 0.0931 mL 0.4656 mL 0.9312 mL 2.3281 mL
    30 mM 0.0776 mL 0.3880 mL 0.7760 mL 1.9401 mL
    40 mM 0.0582 mL 0.2910 mL 0.5820 mL 1.4550 mL
    50 mM 0.0466 mL 0.2328 mL 0.4656 mL 1.1640 mL
    60 mM 0.0388 mL 0.1940 mL 0.3880 mL 0.9700 mL
    80 mM 0.0291 mL 0.1455 mL 0.2910 mL 0.7275 mL
    100 mM 0.0233 mL 0.1164 mL 0.2328 mL 0.5820 mL
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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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