GLPG4970 

GLPG4970 is a potent, selective and orally active salt-inducible kinase 2/3 (SIK2/SIK3) dual inhibitor with IC₅₀ values of 0.3 nM and 0.7 nM. GLPG4970 has weak inhibition of hERG channel with an IC₅₀ of 29 μM. GLPG4970 can decrease TNFα release and increase IL-10 release GLPG4970 can be used for the researches of inflammation and immunology, such as colitis^[1].

GLPG4970 (Compound 8) 对多种脱靶激酶具有抑制作用，其 IC₅₀ 范围为 4 nM 至 292 nM^[1]。
GLPG4970 可诱导 U2OS 细胞中 CRTC3 的核转位，其 EC₅₀ 值为 16 nM^[1]。
GLPG4970 在经脂多糖 (HY-D1056) 刺激的单核细胞和巨噬细胞中，以剂量依赖性方式抑制 TNFα 的释放，其半数抑制浓度 (IC₅₀) 分别为 3.6 nM 和 8.1 nM^[1]。
GLPG4970 在经脂多糖 (HY-D1056) 刺激的单核细胞和巨噬细胞中， 可增加 IL-10 的释放^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

GLPG4970 (Compound 8) (0.5-30 mg/kg，口服，在 LPS 前 15 分钟给药) 可减少经 LPS (HY-D1056) 处理的小鼠的 TNFα 释放，并增加其 IL-10 释放^[1]。
GLPG4970 (3-30 mg/kg，口服，每日两次) 可减缓右旋糖酐硫酸钠 (DSS) 诱导的结肠炎小鼠模型的疾病进展^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

524.58

C₂₉H₃₁F₃N₄O₂

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Kelgtermans H, et al. Structure-Activity Relationship Guided Scaffold Hopping Resulted in the Identification of GLPG4970, a Highly Potent Dual SIK2/SIK3 Inhibitor. J Med Chem. 2025 Aug 14;68(15):16551-16577.  [Content Brief]