A GPR84 antagonist
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GPR84 Antagonist 8

Item No. 43485

Technical Information
Formal Name
2-(1,4-dioxan-2-ylmethoxy)-6,7-dihydro-9-(2-pyridinylmethoxy)-4H-pyrimido[6,1-a]isoquinolin-4-one
CAS Number
1445846-30-9
Synonyms
  • EN 818470
  • G Protein-coupled Receptor 84 Antagonist 8
Molecular Formula
C23H23N3O5
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=C1N(CCC2=C3C=CC(OCC4=NC=CC=C4)=C2)C3=CC(OCC5OCCOC5)=N1
InChi Code
InChI=1S/C23H23N3O5/c27-23-25-22(31-15-19-14-28-9-10-29-19)12-21-20-5-4-18(11-16(20)6-8-26(21)23)30-13-17-3-1-2-7-24-17/h1-5,7,11-12,19H,6,8-10,13-15H2
InChi Key
KSGKMLVYIUJQMZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    GPR84 antagonist 8 is an antagonist of G protein-coupled receptor 84 (GPR84).1 It inhibits calcium mobilization induced by 6-OAU (Item No. 17687) in HEK293 cells expressing human GPR84 and Gα16 (IC50 = 716 nM). GPR84 antagonist 8 (10 µM) inhibits 6-OAU-enhanced phagocytosis of E. coli by primary mouse bone marrow-derived macrophages (BMDMs).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chen, L.-H., Zhang, Q., Xiao, Y.-F., et alPhosphodiesters as GPR84 antagonists for the treatment of ulcerative colitis. J. Med. Chem. 65(5), 3991-4006 (2022).

    2. Recio, C., Lucy, D., Purvis, G.S.D., et alActivation of the immune-metabolic receptor GPR84 enhances inflammation and phagocytosis in macrophages. Front. Immunol. 9, 1419 (2018).