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GLPG1205

Catalog No. T11411 CAS 1445847-37-9

GLPG1205 is a potent, orally active GPR84 (G protein-coupled receptor) antagonist with anti-inflammatory activity. GLPG1205 shows good PK/PD characteristics and can be used to study pulmonary fibrosis.

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GLPG1205, CAS 1445847-37-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 88.00
5 mg	In stock	$ 218.00
10 mg	In stock	$ 372.00
25 mg	In stock	$ 629.00
50 mg	In stock	$ 896.00
100 mg	In stock	$ 1,220.00
1 mL * 10 mM (in DMSO)	In stock	$ 238.00

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Purity: 99.34%

Purity: 95.97%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GLPG1205 is a potent, orally active GPR84 (G protein-coupled receptor) antagonist with anti-inflammatory activity. GLPG1205 shows good PK/PD characteristics and can be used to study pulmonary fibrosis.
In vitro	When GLPG1205 is administered at a concentration of 1 μM for a duration of 5 minutes, it effectively prevents the generation of reactive oxygen species (ROS) triggered by the GPR84 agonist. In TNF-α primed neutrophils, GLPG1205 exhibits strong antagonistic activity against ZQ16-induced ROS, with an IC50 value of 15 nM. Additionally, at a concentration of 0.5 μM, GLPG1205 completely suppresses the ZQ16-induced increase in intracellular calcium levels ([Ca2+]i) in neutrophils[1].
In vivo	GLPG1250 inhibits the increase in MnSOD in lung bronchial epithelial cells and parenchymal macrophages, in the irradiation model. GLPG1205 dose dependently decreases disease activity, histological activity, neutrophil influx and colonic MPO content,in a mouse IBD model. Oral administration of GLPG1250 (30mg/kg; twice daily for 2 weeks, starts from 7 days post-challenge) greatly reduces the Ashcroft score, in idiopathic pulmonary fibrosis model. Oral administration of GLPG1250 (30mg/kg; once daily starts from 18 weeks post irradition) significantly reduces college deposition in the mouse lung[1].

Molecular Weight	378.42
Formula	C22H22N2O4
CAS No.	1445847-37-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 225.0 mg/mL (594.6 mM), Sonication is recommended.

References and Literature

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. 2. F. Vanhoutte, et al. Human safety, pharmacokinetics and pharmacodynamics of the GPR84 antagonist GLPG1205, a potential new approach to treat IBD. J Crohns Colitisournal of Crohns & Colitis, 2015;9(1):5387. 3. L.Saniere, et al. Characterization of GLPG1205 in Mouse Fibrosis Models: A Potent and Selective Antagonist of GPR84 for Treatment of Idiopathic Pulmonary Fibrosis. American Journal of Respiratory and Critical Care Medicine 2019;199:A1046 4. Desrivot J, 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;10(9):1007-1017.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Membrane Protein-targeted Compound Library GPCR Compound Library Clinical Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

GLPG1205 1445847-37-9 Endocrinology/Hormones GPCR/G Protein Others GPR GLPG-1205 GLPG 1205 inhibitor inhibit

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