Chemical Structure : GLPG4970
CAS No.:
GLPG4970
(GLPG-4970)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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524.59
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Formula
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C29H31F3N4O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Kelgtermans H, et al. J Med Chem. 2025 Jul 25. doi: 10.1021/acs.jmedchem.5c01401.
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