2. GPCR/G Protein
  3. GPR84
  4. GLPG1205

GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis. GLPG1205 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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

CAS No. : 1445847-37-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 10 publication(s) in Google Scholar

GLPG1205 Related Antibodies

Top Publications Citing Use of Products

    GLPG1205 purchased from MedChemExpress. Usage Cited in: Cancer Immunol Res. 2026 Jan 20.  [Abstract]

    Representative histogram and average proliferation from five independent biological replicates. Naïve CD8+ T cells were labeled with CFSE, activated, and treated for 72 hours. The results showed that the addition of GPR84 antagonist GLPG1205 (72 h) during activation resulted in a significant, dose-dependent increase in proliferation at 3 μmol/L (39.3%) and 10 μmol/L (71.7%).

    GLPG1205 purchased from MedChemExpress. Usage Cited in: Cancer Immunol Res. 2026 Jan 20.  [Abstract]

    Average tumor volumes and associated spider plots of B16-F10 tumor-bearing mice. Mice were administered a sham treatment or adoptively transferred activated pmel CD8+ T cells pretreated with DMSO or 10 μmol/L GLPG1205. Displayed results are obtained from one significant experiment. The results showed that pmel CD8+ T cells that were activated and treated with 10 μmol/L GLPG1205 prior to adoptive transfer elicited the best antitumor response, significantly better than the DMSO positive control or sham.

    GLPG1205 purchased from MedChemExpress. Usage Cited in: Mol Med. 2025 May 14;31(1):187.  [Abstract]

    WT mice were injected with Con A (15 mg/kg) for 1 h, treated with GLPG1205 or vehicle control by oral gavage, Serum ALT and AST levels were measured. n = 3–7 mice per group. The results showed that compared with the vehicle control group, serum ALT and AST levels were significantly reduced in the GLPG1205-treated mice, indicating that GLPG1205 effectively attenuated Con A-induced liver injury.

    GLPG1205 purchased from MedChemExpress. Usage Cited in: Mol Med. 2025 May 14;31(1):187.  [Abstract]

    WT mice were injected with Con A (15 mg/kg) for 1 h, treated with GLPG1205 or vehicle control by oral gavage. H&E staining was performed to assess liver tissue damage. The results showed that the area of ​​liver injury in the GLPG1205 group was significantly smaller than that in the vehicle control group.

    GLPG1205 purchased from MedChemExpress. Usage Cited in: Mol Med. 2025 May 14;31(1):187.  [Abstract]

    WT mice were injected with Con A (15 mg/kg) for 1 h, and treated with GLPG1205 or vehicle control by oral gavage. Bone marrow-derived macrophages (BMDMs) were pretreated with GLPG1205 for 1 h, followed by Con A treatment at 0 h, 0.5 h, 1 h, and 2 h. Western blotting was used to measure the expression of proteins involved in the STAT3, MAPK, and NF-κB signaling pathways. The results showed that, compared with the GLPG1205 group, the expression levels of p-STAT3, p-ERK, p-JNK, p-p38, and p-p65 were significantly elevated in the vehicle control group (Vehicle group).

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis[1][2]. GLPG1205 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

    Cellular Effect
    Cell Line Type Value Description References
    Neutrophil IC50
    11 nM
    Compound: (S)-36
    Inhibition of embelin-induced migration of human neutrophils preincubated for 30 mins followed by embelin addition and measured after 1 hr by ATPlite luminescence assay
    Inhibition of embelin-induced migration of human neutrophils preincubated for 30 mins followed by embelin addition and measured after 1 hr by ATPlite luminescence assay
    		[PMID: 32902984]
    Neutrophil IC50
    111 nM
    Compound: (S)-36
    Inhibition of embelin-induced migration of rat neutrophils preincubated for 30 mins followed by embelin addition and measured after 1 hr by celltiter-glo assay
    Inhibition of embelin-induced migration of rat neutrophils preincubated for 30 mins followed by embelin addition and measured after 1 hr by celltiter-glo assay
    		[PMID: 32902984]
    Neutrophil IC50
    75 nM
    Compound: (S)-36
    Inhibition of dog neutrophil cell migration
    Inhibition of dog neutrophil cell migration
    		[PMID: 32902984]
    In Vitro

    GLPG1205 (0.5 μM) completely inhibits the ZQ16-induced [Ca2+]i response in neutrophils[1].
    GLPG1205 (1 μM; for 5 min) completely blocks the ROS-response induced by the GPR84-agonist[1].
    GLPG1205 can potently antagonizes ZQ16-induced ROS with an IC50 value of 15 nM in TNF-α primed neutrophils[1].

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

    GLPG1205 Related Antibodies
    In Vivo

    GLPG1250 (orally adminstation; 30mg/kg; twice daily) for 2 weeks, starts from 7 days post-challenge,greatly reduces the Ashcroft score, in idiopathic pulmonary fibrosis model[3].
    GLPG1250 (orally adminstation; 30mg/kg; once daily) starts from 18 weeks post irradition, significantly reduces college deposition in the mouse lung. Additionlly, GLPG1250 inhibits the increase in MnSOD in lung bronchial epithelial cells and parenchymal macrophages, in the irradiation model[3].
    GLPG1205 dose dependently decreases disease activity, histological activity, neutrophil influx and colonic MPO content,in a mouse IBD model[4].

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

    378.42

    Formula

    C22H22N2O4
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C1N=C(OC[C@H]2OCCOC2)C=C3N1CCC4=C3C=CC(C#CC5CC5)=C4
    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 : 250 mg/mL (660.64 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 2.6426 mL 13.2128 mL 26.4257 mL
    5 mM 0.5285 mL 2.6426 mL 5.2851 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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    Concentration
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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

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

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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: 6.25 mg/mL (16.52 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 6.25 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 (62.5 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 6.25 mg/mL (16.52 mM); Clear solution

      This protocol yields a clear solution of ≥ 6.25 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 (62.5 mg/mL) to 900 μL Corn oil, and mix evenly.

    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:  0.5% CMC-Na/saline water

      Solubility: 5 mg/mL (13.21 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  0.5% CMC-Na/1% Tween-80 in Saline water

      Solubility: 16.78 mg/mL (44.34 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
    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 2.6426 mL 13.2128 mL 26.4257 mL 66.0642 mL
    5 mM 0.5285 mL 2.6426 mL 5.2851 mL 13.2128 mL
    10 mM 0.2643 mL 1.3213 mL 2.6426 mL 6.6064 mL
    15 mM 0.1762 mL 0.8809 mL 1.7617 mL 4.4043 mL
    20 mM 0.1321 mL 0.6606 mL 1.3213 mL 3.3032 mL
    25 mM 0.1057 mL 0.5285 mL 1.0570 mL 2.6426 mL
    30 mM 0.0881 mL 0.4404 mL 0.8809 mL 2.2021 mL
    40 mM 0.0661 mL 0.3303 mL 0.6606 mL 1.6516 mL
    50 mM 0.0529 mL 0.2643 mL 0.5285 mL 1.3213 mL
    60 mM 0.0440 mL 0.2202 mL 0.4404 mL 1.1011 mL
    80 mM 0.0330 mL 0.1652 mL 0.3303 mL 0.8258 mL
    100 mM 0.0264 mL 0.1321 mL 0.2643 mL 0.6606 mL
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    GLPG1205 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:

    GLPG12051445847-37-9GLPG 1205GLPG-1205GPR84G protein coupled receptor 84G-protein-coupledreceptoractivationGTPγSbindingassayanti-inflammatoryactivitypulmonaryfibrosisIBDInhibitorinhibitorinhibit

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