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[CAS NO. 1445847-37-9] GLPG1205
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-135303 |
| Brand: | MCE |
| CAS: | 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 |
1 Publications Citing Use of MCE
Summary
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
DMSO : 250 mg/mL ( 660.64 mM ; Need ultrasonic)
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 |
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;
- [2] F. Vanhoutte, et al. Human safety, pharmacokinetics and pharmacodynamics of the GPR84 antagonist GLPG1205, a potential new approach to treat IBD.
- [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] F. Vanhoutte, et al. Human safety, pharmacokinetics and pharmacodynamics
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