GLPG4970 | SIK2/3 inhibitor | Probechem Biochemicals

Chemical Structure : GLPG4970

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GLPG4970 (GLPG-4970)

货号: PC-25118Not For Human Use, Lab Use Only.

GLPG4970 is a highly potent, selective dual SIK2/SIK3 inhibitor with IC50 of 0.3/0.7 nM respectively.

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生物&药学活性

GLPG4970 is a highly potent, selective dual SIK2/SIK3 inhibitor with IC50 of 0.3/0.7 nM respectively.
GLPG4970 shows weak inhibition of hERG channel with an IC50 of 29 μM as assessed using the MPC assay.
GLPG4970 dose-dependently inhibits TNFα release, with an IC50 of 3.6 nM and 8.1 nM, respectively in monocytes and macrophages stimulated with LPS, >4-fold more potent than GLPG3970.
GLPG4970 shows potent inhibition of TNFα production with an IC50 of 83 nM in human whole blood.
GLPG4970 (0.5-30 mg/kg, i.p.) reduced the release of TNFα in a dose-dependent mannerd in in vivo acute LPS challenge model in mice.
GLPG4970 (3, 10, and 30 mg/k, twice daily, orally) is active in reducing disease activity in a mouse DSS-induced model of colitis.

物理化学性质&存储条件

分子量	524.59
分子式	C29H31F3N4O2
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	6-(2-Amino-5-(2,3,3-trimethyl-1,2,3,4-tetrahydroisoquinolin-7-yl)pyridin-3-yl)-8-methoxy-2-(2,2,2-trifluoroethyl)-3,4-dihydroisoquinolin-1(2H)-one

参考文献

1. Kelgtermans H, et al. J Med Chem. 2025 Jul 25. doi: 10.1021/acs.jmedchem.5c01401.

GLPG4970 (GLPG-4970)

生物&药学活性

物理化学性质&存储条件

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GLPG4970 (GLPG-4970)

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物理化学性质&存储条件

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