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

GLPG1205 

Cat. No.: HY-135303
Handling Instructions

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.

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

GLPG1205 Chemical Structure

GLPG1205 Chemical Structure

CAS No. : 1445847-37-9

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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].

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].

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].

Clinical Trial
Molecular Weight

378.42

Formula

C₂₂H₂₂N₂O₄

CAS No.

1445847-37-9

SMILES

O=C1N=C(OC[[email protected]]2OCCOC2)C=C3N1CCC4=C3C=CC(C#CC5CC5)=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

GLPG1205GLPG 1205GLPG-1205GPR84G protein coupled receptor 84G-protein-coupledreceptoractivationGTPγSbindingassayanti-inflammatoryactivitypulmonaryfibrosis, IBDInhibitorinhibitorinhibit

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GLPG1205
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HY-135303
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