GLPG1205 |
Katalog-Nr.GC39385
One-Click Copy Product Info
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GLPG1205 ist ein potenter, selektiver und oral aktiver GPR84-Antagonist (ein G-Protein-gekoppelter Rezeptor) mit einem gÜnstigen PK/PD-Profil.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1445847-37-9
Sample solution is provided at 25 µL, 10mM.
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GLPG1205 is a novel, orally active GPR84 (G-protein-coupled receptor) antagonist. GLPG1205 reduces the release of cytokines (such as IL-8, IL-12, and TNF-α) by inhibiting the GPR84-mediated inflammatory signaling pathway[1-2]. GLPG1205 can be used in research on diseases such as idiopathic pulmonary fibrosis and asthma[3-4].
In vitro, human neutrophils, monocytes, and monocyte-derived macrophages were pretreated with GLPG1205 (0.5-1μM) for 4-5 minutes, followed by stimulation with the GPR84-selective agonist ZQ16 (0.5-1μM). GLPG1205 completely inhibited the ZQ16-induced intracellular Ca²⁺ increase and significantly suppressed the ZQ16-induced reactive oxygen species (ROS) production[5]. THP-1 cells were pretreated with GLPG1205 (20μM) for 20 minutes, which completely inhibited the 6-OAU-induced ROS production[6].
In vivo, C57BL/6J wild-type mice were orally administered GLPG1205 (30mg/kg) one hour after concanavalin A (Con A) injection. GLPG1205 significantly reduced serum ALT and AST levels, decreased the proportion of Kupffer cells and infiltrating monocytes in the liver, and alleviated Con A-induced immune-mediated liver injury[7]. B16-OVA or B16-F10 tumor-bearing mice were orally administered GLPG1205 (30mg/kg) once daily for three days following adoptive T cell transfer. GLPG1205 significantly enhanced the antitumor efficacy of the adoptive CD8⁺ T cells and significantly reduced tumor volume[8].
References:
[1] Timmis H, Van Kaem T, Desrivot J, et al. GLPG1205, a GPR84 Modulator: Safety, Pharmacokinetics, and Pharmacodynamics in Healthy Subjects. Clin Pharmacol Drug Dev. 2021 Sep;10(9):994-1006.
[2] Desrivot J, Van Kaem T, Allamassey L, et al. Effect of GLPG1205, a GPR84 Modulator, on CYP2C9, CYP2C19, and CYP1A2 Enzymes: In Vitro and Phase 1 Studies. Clin Pharmacol Drug Dev. 2021 Sep;10(9):1007-1017.
[3] Donovan C, Thorpe AE, Gomez HM, et al. The GPR84 Antagonist GLPG1205 Reduces Features of Disease in Experimental Severe Asthma. Am J Respir Cell Mol Biol. 2024 May;70(5):424-427.
[4] Strambu IR, Seemayer CA, Fagard LMA, et al. GLPG1205 for idiopathic pulmonary fibrosis: a phase 2 randomised placebo-controlled trial. Eur Respir J. 2023 Mar 2;61(3):2201794.
[5] Schwarzfischer M, Walker MR, Curcio M, et al. Synthetic GPR84 Agonists in Colorectal Cancer: Effective in THP-1 Cells but Ineffective in BMDMs and MC38 Mouse Tumor Models. Int J Mol Sci. 2025 Jan 9;26(2):490.
[6] Sundqvist M, Christenson K, Holdfeldt A, et al. Similarities and differences between the responses induced in human phagocytes through activation of the medium chain fatty acid receptor GPR84 and the short chain fatty acid receptor FFA2R. Biochim Biophys Acta Mol Cell Res. 2018 May;1865(5):695-708.
[7] Zheng Y, Wang Y, Xu Y, et al. Targeting GPR84 to alleviate acute immune-mediated liver injury. Mol Med. 2025 May 14;31(1):187.
[8] Philbrook P, Dean MJ, Sanchez-Pino MD, et al. Medium-Chain Fatty Acid Receptor GPR84 Modulates Cytotoxic CD8 T cells Antitumor Immunity Through Metabolic Reprogramming. Cancer Immunol Res. 2026 Jan 20:10.1158/2326-6066.CIR-25-0695.
| Cell experiment [1]: | |
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Cell lines |
THP-1 cells (human monocytic cell line) |
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Preparation Method |
Undifferentiated human THP-1 cells were incubated with 50ng/mL PMA for 3h, seeded in a 96-well plate, and incubated for 24h. The cells were then incubated with the GLPG1205 (20μM) for 20 min at room temperature. |
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Reaction Conditions |
20μM; 20min. |
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Applications |
GLPG1205 completely inhibited 6-OAU-induced ROS production in THP-1 cells. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6 mice |
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Preparation Method |
For adoptive transfer, OT-I or pmel CD8+ T cells were pre-treated in vitro with 10μM GLPG1205 for 72 hours prior to transfer into tumor-bearing mice. In a therapeutic vaccination model, tumor-bearing mice receiving adoptive T cell transfer were orally administered 30mg/kg GLPG1205 once daily, starting 16 hours post-vaccination |
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Dosage form |
30mg/kg; oral gavage; once daily for 3 days. |
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Applications |
Pre-treatment of antigen-specific CD8+ T cells with GLPG1205 prior to adoptive transfer significantly enhanced their antitumor effect, leading to a significant reduction in tumor volume in both B16-OVA and B16-F10 models. This was associated with a significant increase in the infiltration of antigen-specific CD8+ T cells within the tumor. Orally administered GLPG1205 in combination with therapeutic vaccination also significantly improved antitumor efficacy. |
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References: |
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| Cas No. | 1445847-37-9 | SDF | |
| Canonical SMILES | O=C1N=C(OC[C@H]2OCCOC2)C=C3N1CCC4=C3C=CC(C#CC5CC5)=C4 | ||
| Formula | C22H22N2O4 | M.Wt | 378.42 |
| Löslichkeit | DMSO: 250 mg/mL (660.64 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6426 mL | 13.2128 mL | 26.4257 mL |
| 5 mM | 528.5 μL | 2.6426 mL | 5.2851 mL |
| 10 mM | 264.3 μL | 1.3213 mL | 2.6426 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)