2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. RS 504393

RS 504393 is a selective CCR2 chemokine receptor antagonist (IC50 values are 89 nM and > 100 μM for inhibition of human recombinant CCR2 and CCR1 receptors respectively).

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

CAS No. : 300816-15-3

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Customer Review

Based on 30 publication(s) in Google Scholar

Other Forms of RS 504393:

RS 504393 Related Antibodies

Top Publications Citing Use of Products

30 Publications Citing Use of MCE RS 504393

Cell Migration/Invasion Assay
In Vivo Efficacy Study
Histological Imaging/Staining

    RS 504393 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Aug 7:e03480.  [Abstract]

    After the pre‐treatment of RS504393 (500 nM, 3h), the medium supernatant of OAPS primary decidual cells and aPL‐IgG/β2GPI complex‐stimulated HC primary decidual cells exhibited inhibited chemotactic effects on both THP‐1 and THP‐1‐derived macrophages.

    RS 504393 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2025 Jan 16;135(2):e178198.  [Abstract]

    Administered the CCR2 inhibitor RS504393 (4 mg/kg/d) to Fbn1C1041G/+ mice to inhibit monocyte recruitment from the age of 6 weeks to 26 weeks. Both aortic root and ascending aortic aneurysms as well as related aortic wall pathologies were alleviated following RS504393 administration.

    RS 504393 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2025 Jan 16;135(2):e178198.  [Abstract]

    Administered the CCR2 inhibitor RS504393 (4 mg/kg/d) to Fbn1C1041G/+ mice to inhibit monocyte recruitment from the age of 6 weeks to 26 weeks. Both aortic root and ascending aortic aneurysms as well as related aortic wall pathologies were alleviated following RS504393 administration.

    RS 504393 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2025 Jan 16;135(2):e178198.  [Abstract]

    Administered the CCR2 inhibitor RS504393 (4 mg/kg/d) to Fbn1C1041G/+ mice to inhibit monocyte recruitment from the age of 6 weeks to 26 weeks. RS504393 did not affect body weights and blood pressures in Fbn1C1041G/+ mice, but succeeded in inhibiting Ly6Chi monocyte infiltration and subsequent CX3CR1+ macrophage accumulation without influencing other CX3CR1– cells in thoracic aneurysmal aortas.

    RS 504393 purchased from MedChemExpress. Usage Cited in: Theranostics. 2024 Oct 7;14(17):6543-6559.  [Abstract]

    Quantification of U937 cell migration in a transwell system in response to the CM from 5637 cells (shNC, sh1, and sh1 treated with RS 504393 (2 μM), a CCL2 receptor inhibitor).

    View All CCR Isoform Specific Products:

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    CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    RS 504393 is a selective CCR2 chemokine receptor antagonist (IC50 values are 89 nM and > 100 μM for inhibition of human recombinant CCR2 and CCR1 receptors respectively).

    IC50 & Target[5]

    CCR2

    89 nM (IC50)

    Human α1a receptor

    72 nM (IC50)

    Human α1d receptor

    460 nM (IC50)

    5HT-1a receptor

    1070 nM (IC50)

    In Vitro

    RS 504393 inhibits the MCP-1-induced chemotaxis with an IC50 of 330 nM. RS 504393 treatment suppresses allergen induced β-hexosaminidase release significantly. Without allergen priming, MCP-1 induces mast cell degranulation, which is completely suppressed by RS 504393[4].

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

    RS 504393 Related Antibodies
    In Vivo

    RS504393 (0.3-3 μg) with CCL2 progressively blocks thermal hyperalgesia dose-dependently in mice[1]. RS 504393 (5 mg/kg, i.v.) supresses the elevated numbers of leukocytes and increased total protein content in BALF induced by The LPS. RS504393 significantly down regulates the LPS-induced elevation of IL-1β, PAI-1 mRNA and protein expressions. RS504393 significantly suppresses induced lung edema, protein-rich fluid, polymorphonuclear accumulation and bronchial wall thickening induced by LPS[2]. RS-504393 significantly reduces renal pathology, especially the extensive interstitial fibrosis mediated by decrease in type I collagen synthesis in a UUO model[3].

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

    417.50

    Formula

    C25H27N3O3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1NC2=CC=C(C)C=C2C3(CCN(CCC4=C(C)OC(C5=CC=CC=C5)=N4)CC3)O1
    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 : 10 mg/mL (23.95 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 2.3952 mL 11.9760 mL 23.9521 mL
    5 mM 0.4790 mL 2.3952 mL 4.7904 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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    Volume
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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)

    V1

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    C2

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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:  50% DMSO    15% EtOH    35% PEG300

      Solubility: 31.25 mg/mL (74.85 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1.25 mg/mL (2.99 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: 5 mg/mL (11.98 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 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: 99.72%

    SDS (396 KB)

    COA (252 KB) HNMR (283 KB) RP-HPLC (257 KB) LCMS (339 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [4]

    Isolated mast cells are sensitized by incubation with anti-DNP IgE in RPMI1640 containing 10 ng/mL of murine recombinant IL-3, 10 ng/mL of recombinant SCF, and 5% murine serum. The cells are then washed with HBSS containing 10 ng/mL of murine recombinant IL-3, 10 ng/mL of recombinant SCF, 0.04% BSA, and 10 mM HEPES. Resuspended cells at a concentration of 2 to 8×104 cells/100 μL are transferred into triplicate wells of a 96 well U-bottom plate and allowed to equilibrate at 37°C for 10 minutes before the addition of DNP-albumin or compound 48/80. After 45 minutes, the plate is centrifuged at 290 g for 5 minutes at 4°C. The β-hexosaminidase activity of the culture supernatant is determined using a Published protocol. Fifty-μL aliquots of the supernatant are placed in wells of another 96-well plate together with 100 μL of 2.5 mM p-nitrophenyl-N-acetyl β-d glucosaminide solubilized in 0.04mol/Lcitrate buffer adjusted to pH 4.5 with disodium phosphate. After incubation at 37°C for 90 minutes, the reactions are terminated by addition of 50 μL of 0.4mol/Lglycin adjusted to pH 10.7 with sodium hydroxide. The colored product is measured at 405 nm with a reference filter of 570 nm. The relative release of β-hexosaminidase is defined as the activity in the supernatant of the tested cells divided by the activity in the positive control cell supernatant, multiplied by 100. Compound 48/80 stimulus is used for assay control.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Male C57BL/6J mice (n=30) and male homozygote CCR1, CCR2 and CCR3 knockout mice (n=12, in each phenotype), 6-8 weeks old and weighing 20±2 g. Intranasal administration of PBS or LPS (5 mg/kg) is performed in a volume of 1 mL/kg body weight. C57BL/6J mice are treated with vehicle or RS504393 (5 mg/kg) intraperitoneally 30 min before LPS challenge. Four hours after LPS challenge, mice are terminated by an intraperitoneal injection of an overdose of pentobarbitone. The mice are kept on a 12-h light/dark cycle with access to mice chow and water ad libitum.

    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 2.3952 mL 11.9760 mL 23.9521 mL 59.8802 mL
    5 mM 0.4790 mL 2.3952 mL 4.7904 mL 11.9760 mL
    10 mM 0.2395 mL 1.1976 mL 2.3952 mL 5.9880 mL
    15 mM 0.1597 mL 0.7984 mL 1.5968 mL 3.9920 mL
    20 mM 0.1198 mL 0.5988 mL 1.1976 mL 2.9940 mL
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    RS 504393 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:

    RS 504393300816-15-3RS504393RS-504393CCRCC chemokine receptorInhibitorinhibitorinhibit

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