2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. RS102895

RS102895 is a potent CCR2 antagonist, with an IC50 of 360 nM, and shows no effect on CCR1.

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

RS102895 Chemical Structure

RS102895 Chemical Structure

CAS No. : 300815-41-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 82 In-stock
Solution
10 mM * 1 mL in DMSO USD 82 In-stock
Solid
5 mg USD 75 In-stock
10 mg USD 120 In-stock
25 mg USD 220 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 19 publication(s) in Google Scholar

Other Forms of RS102895:

RS102895 Related Antibodies

Top Publications Citing Use of Products

    RS102895 purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2017 Sep;16(3):3387-3394.  [Abstract]

    Western blot analysis of the protein expression of ERK1/2, p ERK1/2, p38 and p p38 is performed using SDS PAGE.

    View All CCR Isoform Specific Products:

    View All Isoforms
    CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    RS102895 is a potent CCR2 antagonist, with an IC50 of 360 nM, and shows no effect on CCR1.

    IC50 & Target[1]

    CCR2

    360 nM (IC50)

    CCR1

    17800 nM (IC50)

    Human α1a receptor

    130 nM (IC50)

    Human α1d receptor

    320 nM (IC50)

    5HT-1a receptor

    470 nM (IC50)

    In Vitro

    RS102895 is a potent CCR2 antagonist, with an IC50 of 360 nM, and shows no effect on CCR1. RS102895 also inhibits human α1a and α1d receptors, rat brain cortex 5HT1a receptor in cells with IC50s of 130, 320, 470 nM, respectively. RS102895 suppresses wild type and D284N mutant MCP-1 receptor (IC50, 550 nM and 568 nM, respectively), less potently inhibits D284A MCP-1 receptor (IC50, 1892 nM), and has no effects on E291A, E291Q, D284A/E291A or D284N/E291Q (IC50, >100,000 nM)[1]. RS102895 ameliorates the increased extracellular matrix (ECM) protein expression by inhibition of CCR2 at 10 μM, and obviously blocks fibronectin and type IV collagen protein expression in high glucose (HG)-stimulated mesangial cells (MCs) at 1 or 10 μM. RS102895 (10 μM) also abrogates the increased TGF-1 levels in MCs treated with MCP-1[2].

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

    RS102895 Related Antibodies
    In Vivo

    RS102895 (3 g/L) causes progressive decrease in pain threshold in rats with bone cancer pain (BCP) at day 3-9 after surgery via intrathecal injection, but the pain threshold increases after 12 days. RS102895 also potently reverses the pattern of NR2B, nNOS, and SIGIRR expression in spinal cord[3].

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

    390.40

    Formula

    C21H21F3N2O2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1NC2=CC=CC=C2C3(CCN(CCC4=CC=C(C(F)(F)F)C=C4)CC3)O1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 250 mg/mL (640.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 50 mg/mL (128.07 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5615 mL 12.8074 mL 25.6148 mL
    5 mM 0.5123 mL 2.5615 mL 5.1230 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • 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: ≥ 2.5 mg/mL (6.40 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    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: 99.97%

    COA (247 KB) HNMR (271 KB) LCMS (95 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    Transfected mesangial cells (MCs) are serum restricted for 24 h, after which the medium is replaced by serum-free DMEM containing normal glucose (NG; 5.6 mM), NG+Mannitol (NG+M; 24.4 mM), or high glucose (HG; 30 mM). In addition, nontransfected MCs are cultured under NG, NG+M, or HG with or without RS102895 or anti-TGF-1 antibody (25 μg/mL). Nontransfected MCs are also exposed to medium containing recombinant human MCP-1 (10 ng/mL) or recombinant human TGF-1 (2 ng/mL). At 24 h after the media change, cells are harvested and the conditioned culture media are collected[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    Rats[3]
    CCR2 antagonist RS102895 is dissolved in DMSO. Rats receive daily intrathecal injection of either RS102895 (3 g/L) 10 μL or 10 % DMSO 10 μL between 9 and 20 days after operation. All rats are randomLy divided into five groups (n = 10 per group): Sham group, Sham + RS102895 group, BCP group, BCP + RS102895 group, and BCP + DMSO group. Rats are sacrificed 20 days after operation and the tissue samples from the L4-L5 spinal cord segments are rapidly removed and immediately frozen in liquid nitrogen and stored at −80°C until use for RT-PCR and Western blot[3].

    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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 2.5615 mL 12.8074 mL 25.6148 mL 64.0369 mL
    5 mM 0.5123 mL 2.5615 mL 5.1230 mL 12.8074 mL
    10 mM 0.2561 mL 1.2807 mL 2.5615 mL 6.4037 mL
    15 mM 0.1708 mL 0.8538 mL 1.7077 mL 4.2691 mL
    20 mM 0.1281 mL 0.6404 mL 1.2807 mL 3.2018 mL
    25 mM 0.1025 mL 0.5123 mL 1.0246 mL 2.5615 mL
    30 mM 0.0854 mL 0.4269 mL 0.8538 mL 2.1346 mL
    40 mM 0.0640 mL 0.3202 mL 0.6404 mL 1.6009 mL
    50 mM 0.0512 mL 0.2561 mL 0.5123 mL 1.2807 mL
    60 mM 0.0427 mL 0.2135 mL 0.4269 mL 1.0673 mL
    80 mM 0.0320 mL 0.1601 mL 0.3202 mL 0.8005 mL
    100 mM 0.0256 mL 0.1281 mL 0.2561 mL 0.6404 mL
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    RS102895 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:

    RS102895300815-41-2RS 102895RS-102895CCRCC chemokine receptorInhibitorinhibitorinhibit

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