GLPG4471 (GLPG-4471)

Chemical Structure : GLPG4471

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货号: PC-25433Not For Human Use, Lab Use Only.

GLPG4471 (GLPG-4471) is a a potent and selective IRAK4 inhibitor with IC50 of 1.7 nM, potently inhibits CL097-induced TNFα in PBMCs with IC50 of 39.4 nM.

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250 mg		Get quote

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生物&药学活性

GLPG4471 (GLPG-4471) is a a potent and selective IRAK4 inhibitor with IC50 of 1.7 nM, potently inhibits CL097-induced TNFα in PBMCs with IC50 of 39.4 nM.
GLPG4471 potently inhibits the CL097-induced secretion of TNFα and IFNα in human whole blood stimulated with IC50 of 17.1 and 28.0 nM respectively.
GLPG4471 inhibits mouse IRAK4 with IC50 of 2.4 nM.
GLPG4471 displays excellent kinome selectivity against a panel of 369 kinases at 1 uM.
GLPG4471 (30  mg/kg, b.i.d, ora) lexhibited dose-dependent activity in vivo in the CIA mouse model of rheumatoid arthritis.

物理化学性质&存储条件

分子量	410.47
分子式	C22H26N4O4
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
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-cyclopropyl-N-(2-(3-hydroxy-3-methylbutyl)-6-methoxypyrazolo[1,5-a]pyridin-5-yl)-2-oxo-1,2-dihydropyridine-3-carboxamide

参考文献

1. Mammoliti O, et al. Bioorg Med Chem Lett. 2025 Aug 23:130386.