An inhibitor of SIK1-3 and RIPK2
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GLPG3970

Item No. 45730

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3,4-dihydro-8-methoxy-6-[7-[2-(4-morpholinyl)ethoxy]imidazo[1,2-a]pyridin-3-yl]-2-(2,2,2-trifluoroethyl)-1(2H)-isoquinolinone
CAS Number
2403733-82-2
Molecular Formula
C25H27F3N4O4
Formula Weight
504.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥ 10 mg/mlEthanol: Soluble: ≥ 10 mg/ml
SMILES
O=C1C2=C(C=C(C=C2OC)C3=CN=C4N3C=CC(OCCN5CCOCC5)=C4)CCN1CC(F)(F)F
InChi Code
InChI=1S/C25H27F3N4O4/c1-34-21-13-18(12-17-2-4-31(16-25(26,27)28)24(33)23(17)21)20-15-29-22-14-19(3-5-32(20)22)36-11-8-30-6-9-35-10-7-30/h3,5,12-15H,2,4,6-11,16H2,1H3
InChi Key
XASOHFCUIQARJT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    5 mg

    $49

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    10 mg

    $83

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    25 mg

    $159

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    50 mg

    $245

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    Product Description

    GLPG3970 is an inhibitor of salt-inducible kinase 1 (SIK1), SIK2, SIK3, and receptor-interacting serine/threonine kinase 2 (RIPK2; IC50s = 282.8, 7.8, 3.8, and 78.4 nM, respectively).1 It is selective for SIK1, SIK2, SIK3, and RIPK2 over a panel of 371 other kinases at 1 µM. GLPG3970 reduces the levels of TNF-α and IL-12 and increases the level of IL-10 in LPS-stimulated primary human monocytes and whole blood. It decreases disease severity in a mouse model of colitis induced by dextran sodium sulfate (DSS) when administered at a dose of 30 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Peixoto, C., Joncour, A., Temal-Laib, T., et al. Discovery of clinical candidate GLPG3970: A potent and selective dual SIK2/SIK3 inhibitor for the treatment of autoimmune and inflammatory diseases. J. Med. Chem. 67(7), 5233-5258 (2024).