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TargetMol - Model GLPG3312 -Selective Pan-SIK Inhibitor
GLPG3312 is a selective and potent pan-SIK inhibitor with the advantage of oral activity, with IC50=0.6-2.0 nM for SIK1, SIK2 and SIK3, and exhibits anti-inflammatory and immunomodulatory activity in both human primary myeloid cells and mouse models.
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- Targets&IC50
- Monocyte-derived macrophages (MdMs):?34 nM, Primary CD14? monocytes(human):?17 nM
- In vitro
- In LPS (100 ng/mL)-stimulated human primary CD14? monocytes and monocyte-derived macrophages (MdMs),GLPG3312 inhibited TNFα release in monocytes(IC50 17 nM) and in MdMs(IC50 34 nM). At a concentration of 20 μM, GLPG3312 enhanced IL-10 secretion by 14.8-fold in monocytes and 2.8-fold in MdMs. Cells were preincubated with the compound for 1 hour before LPS stimulation, and cytokine levels were measured at 4 hours for monocytes and at 2 and 20 hours for IL-10 and TNFα, respectively, in MdMs[1].
- In vivo
- In Balb/c mice, GLPG3312 was administered p.o. at 0.3, 1, or 3 mg/kg, followed by i.p. LPS (100?μg) 15?min later. Plasma cytokines measured at 1.5?h post-LPS showed TNFα inhibition of 27.0%, 57.2%, and 77.5%, respectively, and IL-10 increases of 1.3-, 2.4-, and 3.1-fold at the same doses. GLPG3312 also exhibited favorable PK, with oral bioavailability of 60% in mice, 41.4% in rats (5?mg/kg), and 45.5% in dogs (30?mg/kg), along with low CL and acceptable t1/2[1].
- Synonyms: GLPG 3312
- Molecular Weight: 453.44
- Formula: C23H21F2N5O3
- Cas No.: 2340388-72-7
- Smiles: O=C(NC1CC1)C2=C(OC)C=C(C=C2OC(F)F)N3C=NC=4C=C(C=CC43)C=5C=NN(C5)C
- Color: White
- Appearance: Solid