2. GPCR/G Protein
  3. Adenosine Receptor
  4. LUF6000

LUF6000 is an orally active allosteric modulator of the A3 adenosine receptor. LUF6000 has potent anti-inflammatory effect.

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

LUF6000 Chemical Structure

LUF6000 Chemical Structure

CAS No. : 890087-21-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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 USD 436 In-stock
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10 mM * 1 mL in DMSO USD 436 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

LUF6000 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE LUF6000

WB

    LUF6000 purchased from MedChemExpress. Usage Cited in: Mediators Inflamm. 2014;2014:708746.  [Abstract]

    LUF6000 down-regulates the A3AR and key inflammatory proteins. Protein analysis is performed using WB analysis. LUF6000 downregulates A3AR expression levels in the PBMCs of OA-induced rats (a). Jak-2 and STAT-1 are downregulated upon LUF6000 administration (b).

    View All Adenosine Receptor Isoform Specific Products:

    View All Isoforms
    Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    LUF6000 is an orally active allosteric modulator of the A3 adenosine receptor. LUF6000 has potent anti-inflammatory effect[1][2].

    In Vitro

    Modulatory effect of 10 μM LUF6000 on Cl-IB-MECA-induced [35S]GTPγS binding in assays with HEK 293 cell membranes expressing human, dog, rabbit, or mouse A3 adenosine receptors with EC50 ranging from 39 to 172 nM[1].

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

    LUF6000 Related Antibodies
    In Vivo

    LUF6000 induces anti-inflammatory effect in 3 experimental animal models of rat adjuvant induced arthritis, monoiodoacetate induced osteoarthritis, and concanavalin A induced liver inflammation in mice[2].

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

    411.33

    Formula

    C22H20Cl2N4
    CAS No.
    Appearance

    Solid

    Color

    Light brown to brown

    SMILES

    ClC1=CC(NC2=NC3=C(C=CC=C3)C4=C2NC(C5CCCCC5)=N4)=CC=C1Cl
    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 : 14.29 mg/mL (34.74 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 2.4311 mL 12.1557 mL 24.3114 mL
    5 mM 0.4862 mL 2.4311 mL 4.8623 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)

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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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    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: ≥ 1.43 mg/mL (3.48 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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.
    • Protocol 2

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

      Solubility: 1.43 mg/mL (3.48 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.43 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 (14.3 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
    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 2.4311 mL 12.1557 mL 24.3114 mL 60.7785 mL
    5 mM 0.4862 mL 2.4311 mL 4.8623 mL 12.1557 mL
    10 mM 0.2431 mL 1.2156 mL 2.4311 mL 6.0778 mL
    15 mM 0.1621 mL 0.8104 mL 1.6208 mL 4.0519 mL
    20 mM 0.1216 mL 0.6078 mL 1.2156 mL 3.0389 mL
    25 mM 0.0972 mL 0.4862 mL 0.9725 mL 2.4311 mL
    30 mM 0.0810 mL 0.4052 mL 0.8104 mL 2.0259 mL
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    LUF6000 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:

    LUF6000890087-21-5LUF 6000LUF-6000Adenosine ReceptorP1 receptororalallostericanti-inflammatoryarthritisosteoarthritisInhibitorinhibitorinhibit

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