GLPG1205 | GPR84 antagonist | Probechem Biochemicals

Chemical Structure : GLPG1205

CAS No.: 1445847-37-9

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GLPG1205 (GLPG 1205, GLPG-1205)

货号: PC-72356Not For Human Use, Lab Use Only.

GLPG1205 is a potent and selective GPR84 inhibitor (negative allosteric modulator) with IC50 of 54 nM (hGPR84).

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5 mg	￥2380	In stock
10 mg	￥3780	In stock
25 mg	￥5980	In stock
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100 mg		Get quote

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生物&药学活性

GLPG1205 is a potent and selective GPR84 inhibitor (negative allosteric modulator) with IC50 of 54 nM (hGPR84).
GLPG1205 is fully selective over close homologs GPR43 (FFA2R) and GPR41 (FFA3R) and >100-fold selective over 123 other GPCRs on a Millipore GPCR Profiler panel.
GLPG1205 exhibits high potency in human and rat neutrophil assay with IC50 of 11 nM and 111 nM, respectively.
GLPG1205 (once-daily doses of 3 and 10 mg/kg) reduced disease activity index score and neutrophil infiltration in a mouse dextran sodium sulfate-induced chronic inflammatory bowel disease model, with efficacy similar to positive-control compound sulfasalazine.

物理化学性质&存储条件

分子量	378.428
分子式	C22H22N2O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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Solubility	10 mM in DMSO
Chemical Name/SMILES	9-Cyclopropylethynyl-2-(( S)-1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1- a]isoquinolin-4-one

参考文献

1. Labéguère F, et al. J Med Chem. 2020 Nov 25;63(22):13526-13545.

GLPG1205 (GLPG 1205, GLPG-1205)

生物&药学活性

物理化学性质&存储条件

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GLPG1205 (GLPG 1205, GLPG-1205)

生物&药学活性

物理化学性质&存储条件

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