[CAS NO. 1445847-37-9] GLPG1205

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PRODUCTS SPECIFICATIONS [1445847-37-9]

Catalog

HY-135303

Brand

MCE

CAS

1445847-37-9

DESCRIPTION [1445847-37-9]

Overview

MDL	-
Molecular Weight	378.42
Molecular Formula	C22H22N2O4
SMILES	O=C1N=C(OC[C@H]2OCCOC2)C=C3N1CCC4=C3C=CC(C#CC5CC5)=C4

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

1 Publications Citing Use of MCE

[1]J Med Chem. 2022 Feb 23.

Summary

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 [Ca ²⁺ ]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 IC ₅₀ value of 15 nM in TNF-α primed neutrophils ^[1] .

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

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] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01887106	Galapagos NV	Healthy	June 2013	Phase 1
NCT02143856	Galapagos NV	Healthy	May 2014	Phase 1
NCT04704739	Galapagos NV	Healthy	January 13, 2021	Phase 1
NCT03725852	Galapagos NV	Idiopathic Pulmonary Fibrosis	September 27, 2018	Phase 2
NCT04532567	Galapagos NV	Healthy	August 18, 2020	Phase 1
NCT02337608	Galapagos NV	Ulcerative Colitis	December 2014	Phase 2
NCT02623296	Galapagos NV	Healthy	October 2015	Phase 1
NCT03102567	Galapagos NV	Healthy\|Elderly	October 18, 2016	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL ( 660.64 mM ; Need ultrasonic)

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
10 mM	0.2643 mL	1.3213 mL	2.6426 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

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
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 6.25 mg/mL (16.52 mM); Clear solution
3.

Add each solvent one by one: 0.5% CMC-Na /saline water

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

* All of the co-solvents are available by MCE.