A GPR84 antagonist
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GLPG1205

Item No. 33185

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
9-(2-cyclopropylethynyl)-2-[(2S)-1,4-dioxan-2-ylmethoxy]-6,7-dihydro-4H-pyrimido[6,1-a]isoquinolin-4-one
CAS Number
1445847-37-9
Molecular Formula
C22H22N2O4
Formula Weight
378.4
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=C1N2C(C3=CC=C(C#CC4CC4)C=C3CC2)=CC(OC[C@@H]5COCCO5)=N1
InChi Code
InChI=1S/C22H22N2O4/c25-22-23-21(28-14-18-13-26-9-10-27-18)12-20-19-6-5-16(4-3-15-1-2-15)11-17(19)7-8-24(20)22/h5-6,11-12,15,18H,1-2,7-10,13-14H2/t18-/m0/s1
InChi Key
IRBAWVGZNJIROV-SFHVURJKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Cayman Chemical
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    Product Description

    GLPG1205 is a G protein-coupled receptor 84 (GPR84) antagonist.1 It inhibits GTPγS binding induced by 3,3’-diindolylmethane (DIM) in cells overexpressing human GPR84 (IC50 = 54 nM). GLPG1205 inhibits embelin-induced chemotaxis of isolated human neutrophils (IC50 = 11 nM). In vivo, GLPG1205 (3 mg/kg) reduces body weight loss and rectal bleeding and improves stool consistency in a rat model of colitis induced by dextran sulfate sodium (DSS; Item No. 23250).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Labéguère, F., Dupont, S., Alvey, L., et al. Discovery of 9-cyclopropylethynyl-2-((S)-1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one (GLPG1205), a unique GPR84 negative allosteric modulator undergoing evaluation in a phase II clinical trial. J. Med. Chem. 63(22), 13526-13545 (2020).