GLPG1205
Based on 10 publication(s) in Google Scholar
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.
- Purity: 99.94%
- CAS No.: 1445847-37-9
- Formula: C22H22N2O4
- Molecular Weight:378.42
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) GLPG1205
More- Cancer Immunol Res. 2026 Jan 20. [Abstract]
- J Med Chem. 2022 Mar 10;65(5):3991-4006. [Abstract]
- Mol Med. 2025 May 14;31(1):187. [Abstract]
- Liver Int. 2025 Sep;45(9):e70270. [Abstract]
- Int J Mol Sci. 2025 Jan 9;26(2):490. [Abstract]
- Int Immunopharmacol. 2025 Jul 21:163:115190. [Abstract]
- Am J Physiol Endocrinol Metab. 2025 Apr 2. [Abstract]
- Universidad de Córdoba. 2025.
- Patent. US20240358705A1.
- Patent. US20240217911A1.
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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Bio/Physico-chemical Assay
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Histological Imaging/Staining
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WB
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Neutrophil | IC50 |
11 nM
Compound: (S)-36
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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
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[PMID: 32902984] |
| Neutrophil | IC50 |
111 nM
Compound: (S)-36
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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
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[PMID: 32902984] |
| Neutrophil | IC50 |
75 nM
Compound: (S)-36
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Inhibition of dog neutrophil cell migration
Inhibition of dog neutrophil cell migration
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[PMID: 32902984] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1445847-37-9
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Appearance Solid
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Molecular Weight 378.42
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Formula C22H22N2O4
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Color Light yellow to yellow
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SMILES
O=C1N=C(OC[C@H]2OCCOC2)C=C3N1CCC4=C3C=CC(C#CC5CC5)=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (10)
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Journal Impact Factor
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Most Recent
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Cancer Immunol Res
Medium-Chain Fatty Acid Receptor GPR84 Modulates Cytotoxic CD8 T cells Antitumor Immunity Through Metabolic Reprogramming. [Abstract]2026 Jan 20. PMID: 41557755
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.
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J Med Chem
2022 Mar 10;65(5):3991-4006. PMID: 35195005 -
Mol Med
2025 May 14;31(1):187. PMID: 40369402
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).
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Liver Int
Medium-Chain Fatty Acids Ameliorate Liver Fibrosis by Phosphorylating Hepatic Stellate Cell Forkhead Box Protein O1. [Abstract]2025 Sep;45(9):e70270. PMID: 40778789 -
Int J Mol Sci
Synthetic GPR84 Agonists in Colorectal Cancer: Effective in THP-1 Cells but Ineffective in BMDMs and MC38 Mouse Tumor Models. [Abstract]2025 Jan 9;26(2):490. PMID: 39859206 -
Int Immunopharmacol
A novel GPR84 antagonist attenuates diabetic lung injury by inhibiting pyroptosis via the cGAS-STING pathway in pulmonary vascular endothelial cells. [Abstract]2025 Jul 21:163:115190. PMID: 40695150 -
Am J Physiol Endocrinol Metab
Central lipid sensing pathways contribute to the control of puberty and its alterations in conditions of obesity. [Abstract]2025 Apr 2. PMID: 40172224 -
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Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Sundqvist M, 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. [Content Brief]
[4]. F. Vanhoutte, et al. Human safety, pharmacokinetics and pharmacodynamics
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 |