GPR183 antagonist-2 (Compound 32) is a selective GPR183 antagonist with good water solubility and excellent pharmacokinetic properties. GPR183 antagonist-2 significantly reduced the swelling of paws and joints and the gene expression of proinflammatory cytokines (MCP-1, MMPs and VEGF) in a collagen-induced arthritis (CIA) mouse model in a dose-dependent manner. GPR183 antagonist-2 can be used in the study of autoimmune diseases.

Physicochemical Properties

CAS #	2924063-98-7
Appearance	White to off-white solid powder
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

References

[1].Discovery of a First-in-Class GPR183 Antagonist for the Potential Treatment of Rheumatoid Arthritis. J Med Chem. 2023 Dec 14;66(23):15926-15943.

Solubility Data

Solubility (In Vitro)

DMSO :~100 mg/mL (~231.28 mM; with sonication (<80°C))

Solubility (In Vivo)

Solubility in Formulation 1: 5 mg/mL (11.56 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared,you can add 100 μL of 50.0 mg/mL clear DMSO stock solution and add it to 900 μL corn oil and mix well.  (Please use freshly prepared in vivo formulations for optimal results.)