2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. REV-ERB
  4. SR8278

SR8278 is a REV-ERBα antagonist and inhibits the REV-ERBα transcriptional repression activity with an EC50 of 0.47 μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm. SR8278 also can be used for the research of Duchenne muscular dystrophy and Alzheimer's disease.

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

SR8278 Chemical Structure

SR8278 Chemical Structure

CAS No. : 1254944-66-5

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 165 In-stock
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10 mM * 1 mL in DMSO USD 165 In-stock
Solid
5 mg USD 150 In-stock
10 mg USD 240 In-stock
25 mg USD 510 In-stock
50 mg USD 810 In-stock
100 mg USD 1290 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

SR8278 Related Antibodies

Top Publications Citing Use of Products

    SR8278 purchased from MedChemExpress. Usage Cited in: In Vitro Cell Dev Biol Anim. 2023 Feb 15.  [Abstract]

    SR8278 promotes the expression of ALPL, BSP, OPN, RUNX2, and OSX signifcantly in OCCM-30 cells.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    SR8278 is a REV-ERBα antagonist and inhibits the REV-ERBα transcriptional repression activity with an EC50 of 0.47 μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm. SR8278 also can be used for the research of Duchenne muscular dystrophy and Alzheimer's disease[1][2][3].

    IC50 & Target

    EC50: 0.47 μM (REV-ERBα)[1].
    In Vitro

    SR8278 has REV-ERBα transcriptional repression inhibitory activity with an EC50 of 0.47μM[1].

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

    SR8278 Related Antibodies
    In Vivo

    SR8278 (slow microinjection; 20 μg/mouse) exerts antidepressant and anxiolytic effects in a circadian time-dependent manner in 6-OHDA-lesioned mice and restores the circadian rhythm of mood-related behaviors[1].
    ? ? SR8278 (slow microinjection; 20 μg/mouse) restores the binding activities of REV-ERBα and NURR1 to the tyrosine hydroxylase promoter and the induction of enrichment of the R/N motif, recognized by REV-ERBα and NURR1[1].

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

    Animal Model: 6-OHDA-lesioned mice[1]
    Dosage: 20 μg/mouse
    Administration: slow microinjection; 20 μg/mouse
    Result: Recovered mood-related behavioral deficits shown in 6-OHDA-lesioned mice.
    Altered remaining DAergic neuron specific transcription levels of REV-ERBα and Nurr1 in the VTA.
    Restored antagonistic crosstalk of REV-ERBα and NURR1 binding activity to TH promoter and TH protein levels in VTA.
    Induced enrichments of REV-ERBα and NURR1 binding motifs at dawn.
    Molecular Weight

    361.48

    Formula

    C18H19NO3S2
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    CSC1=CC=C(C(N2C(C(OCC)=O)CC(C=CC=C3)=C3C2)=O)S1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (276.64 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 2.7664 mL 13.8320 mL 27.6640 mL
    5 mM 0.5533 mL 2.7664 mL 5.5328 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (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 (6.92 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 (6.92 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 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)

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    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: 99.76%

    COA (251 KB) HNMR (280 KB) LCMS (268 KB)

    Handling Instructions (2659 KB)
    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.7664 mL 13.8320 mL 27.6640 mL 69.1601 mL
    5 mM 0.5533 mL 2.7664 mL 5.5328 mL 13.8320 mL
    10 mM 0.2766 mL 1.3832 mL 2.7664 mL 6.9160 mL
    15 mM 0.1844 mL 0.9221 mL 1.8443 mL 4.6107 mL
    20 mM 0.1383 mL 0.6916 mL 1.3832 mL 3.4580 mL
    25 mM 0.1107 mL 0.5533 mL 1.1066 mL 2.7664 mL
    30 mM 0.0922 mL 0.4611 mL 0.9221 mL 2.3053 mL
    40 mM 0.0692 mL 0.3458 mL 0.6916 mL 1.7290 mL
    50 mM 0.0553 mL 0.2766 mL 0.5533 mL 1.3832 mL
    60 mM 0.0461 mL 0.2305 mL 0.4611 mL 1.1527 mL
    80 mM 0.0346 mL 0.1729 mL 0.3458 mL 0.8645 mL
    100 mM 0.0277 mL 0.1383 mL 0.2766 mL 0.6916 mL
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    SR8278 Related Classifications

    Help & FAQs
    • 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.

    Keywords:

    SR82781254944-66-5SR 8278SR-8278REV-ERBREV-ERBαmetabolismbiological rhythmDuchenne muscular dystrophyAlzheimer's diseaseneurosurgeryInhibitorinhibitorinhibit

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