| Bioactivity | GPR84 antagonist 3 (compound 42) is a potent GPR84 (G-protein-coupled receptor 84) antagonist. GPR84 antagonist 3 inhibits GTPγS, with a pIC50 of 8.28. GPR84 antagonist 3 has a favorable pharmacokinetic profile suitable[1]. |
| Target | pIC50: 8.28 ± 0.11 (GTPγS) |
| Invitro | GPR84 antagonist 3 (compound 42) displays no ability to block the actions of the C3 fatty acid propionate at either FFAR2 or FFAR3 when tested at 10 μM[1] |
| In Vivo | GPR84 antagonist 3 (compound 42) (1 mg/kg (IV), 10 mg/kg (Orally); once) has a good elimination half-life (2.51 h), moderate rate of clearance, and bioavailability[1]. Animal Model: |
| Name | GPR84 antagonist 3 |
| CAS | 2815263-05-7 |
| Formula | C29H27N5O |
| Molar Mass | 461.56 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Mahindra A, et al. Investigating the Structure-Activity Relationship of 1,2,4-Triazine G-Protein-Coupled Receptor 84 (GPR84) Antagonists. J Med Chem. 2022 Aug 10. |