1. GPCR/G Protein Immunology/Inflammation
  2. CCR
  3. Bindarit

Bindarit (AF2838) is a selective inhibitor of the monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7, and MCP-2/CCL8, and no effect on other CC and CXC chemokines such as MIP-1α/CCL3, MIP-1β/CCL4, MIP-3/CCL23. Bindarit also has anti-inflammatory activity.

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

CAS No. : 130641-38-2

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10 mM * 1 mL in DMSO
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Customer Review

Based on 29 publication(s) in Google Scholar

Top Publications Citing Use of Products
WB
RT-PCR
Histological Imaging/Staining

    Bindarit purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2024 Oct;14(10):4544-4559.

    Bindarit (300 μM) significantly inhibited CCL2 expression in ChP epithelial cells stimulated with LPS at protein levels.

    Bindarit purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2024 Oct;14(10):4544-4559.

    Bindarit (300 μM) exhibited a notable inhibition of M1 markers CD86 and iNOS expression and the proinflammatory cytokines TNF-α, IL-1β, and GM-CSF in macrophages.

    Bindarit purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2024 Oct;14(10):4544-4559.

    Bindarit (30 mg/kg; i.p.; every 12 h) significantly reduced the ventriculomegaly and CSF secretion rate induced by IVH in PHH rats.

    Bindarit purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2021 Sep;28(9):2616-2633.  [Abstract]

    Bindarit (100 μM; 37 ℃; 3 h) increased the levels of pBTK in B cells from C57BL/6J mice.

    Bindarit purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2021 Sep;28(9):2616-2633.  [Abstract]

    Bindarit (100 μM; 37 ℃; 3 h) increased the levels of pPI3K, pAKT and pS6 in splenic B cells of C57BL/6J mice.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Bindarit (AF2838) is a selective inhibitor of the monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7, and MCP-2/CCL8, and no effect on other CC and CXC chemokines such as MIP-1α/CCL3, MIP-1β/CCL4, MIP-3/CCL23. Bindarit also has anti-inflammatory activity[1].

    IC50 & Target

    MCP-1/CCL2, MCP-3/CCL7, and MCP-2/CCL8[1]

    In Vitro

    Bindarit (10-300 μM; 48 hours) at 100 μM and 300 μM significantly inhibits platelet derived growth factor-BB (PDGF-BB)-induced rat VSMCs proliferation by 27% and 42%, respectively[1].

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

    Cell Viability Assay[1]

    Cell Line: VSMC cells
    Concentration: 10 μM, 30 μM, 100 μM, 300 μM
    Incubation Time: 48 hours
    Result: Inhibited PDGF-BB-induced rat VSMCs proliferation.
    In Vivo

    Bindarit (50 mg/kg; oral administration; every day; for 4 months, 6 months, 8 months; NZB/W F1 female mice) delays the onset of proteinuria and significantly protects from renal function impairment. Bindarit completely prevents monocyte chemoattractant protein (MCP-1) up-regulation[2].

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

    Animal Model: NZB/W F1 female mice ( two months of age)[2]
    Dosage: 50 mg/kg
    Administration: Oral administration; every day; for 4 months, 6 months, 8 months
    Result: Delayed the onset of proteinuria and significantly protected from renal function impairment.
    Clinical Trial
    Molecular Weight

    324.37

    Formula

    C19H20N2O3

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC(OCC1=NN(CC2=CC=CC=C2)C3=C1C=CC=C3)(C)C(O)=O

    Structure Classification
    Initial Source
    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 : ≥ 46 mg/mL (141.81 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.0829 mL 15.4145 mL 30.8290 mL
    5 mM 0.6166 mL 3.0829 mL 6.1658 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)

    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: ≥ 2.67 mg/mL (8.23 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.67 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (26.7 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: ≥ 2.67 mg/mL (8.23 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.67 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (26.7 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.

    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: 5 mg/mL (15.41 mM); Clear 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 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: 99.59%

    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 3.0829 mL 15.4145 mL 30.8290 mL 77.0725 mL
    5 mM 0.6166 mL 3.0829 mL 6.1658 mL 15.4145 mL
    10 mM 0.3083 mL 1.5414 mL 3.0829 mL 7.7072 mL
    15 mM 0.2055 mL 1.0276 mL 2.0553 mL 5.1382 mL
    20 mM 0.1541 mL 0.7707 mL 1.5414 mL 3.8536 mL
    25 mM 0.1233 mL 0.6166 mL 1.2332 mL 3.0829 mL
    30 mM 0.1028 mL 0.5138 mL 1.0276 mL 2.5691 mL
    40 mM 0.0771 mL 0.3854 mL 0.7707 mL 1.9268 mL
    50 mM 0.0617 mL 0.3083 mL 0.6166 mL 1.5414 mL
    60 mM 0.0514 mL 0.2569 mL 0.5138 mL 1.2845 mL
    80 mM 0.0385 mL 0.1927 mL 0.3854 mL 0.9634 mL
    100 mM 0.0308 mL 0.1541 mL 0.3083 mL 0.7707 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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    Product Name:
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    Cat. No.:
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