For research use only. Not for therapeutic Use.
R243 is a potent and selective CCR8 antagonist. R243 inhibits CCL1/CCR8 interaction and inhibits CCR8 signaling and chemotaxis. R243 has antinociceptive and anti-inflammatory effects[1][2].
R243 has CCR8-antagonistic effects on CCL1-induced Ca2+ flux and CCL1-driven peritoneal macrophages aggregation[1].
R243 attenuates secretion of TNF-α, IL-6, and most strikingly IL-10 from wild-type peritoneal macrophages (WT PMφ)[1].
R243-treated WT PMφ shows suppressed c-jun N-terminal kinase activity and NF-κB signaling after lipopolysaccharide (LPS) treatment when compared with WT PMφ[1].
R243 (0.1-1 mg/kg; intraperitoneal injection; once; male Swiss mice) treatment inhibits the analgesic effect evoked by CCL1 in a dose-dependent manner[2].
| Catalog Number | I015355 |
| CAS Number | 688352-84-3 |
| Synonyms | 7-[2-(1-adamantyloxy)ethyl]-6,8-dihydro-[1,3]dioxolo[4,5-g][1,3]benzoxazine |
| Molecular Formula | C21H27NO4 |
| Purity | ≥95% |
| InChI | InChI=1S/C21H27NO4/c1(2-26-21-8-14-3-15(9-21)5-16(4-14)10-21)22-11-17-6-19-20(25-13-24-19)7-18(17)23-12-22/h6-7,14-16H,1-5,8-13H2 |
| InChIKey | JJMLDSFDOODCIR-UHFFFAOYSA-N |
| SMILES | C1C2CC3CC1CC(C2)(C3)OCCN4CC5=CC6=C(C=C5OC4)OCO6 |
| Reference | [1]. Tomoyuki Oshio, et al. Chemokine Receptor CCR8 Is Required for Lipopolysaccharide-Triggered Cytokine Production in Mouse Peritoneal Macrophages. PLoS One. 2014 Apr 8;9(4):e94445. [2]. Mario García-Domínguez, et al. The Systemic Administration of the Chemokine CCL1 Evokes Thermal Analgesia in Mice Through the Activation of the Endocannabinoid System. Cell Mol Neurobiol. 2019 Nov;39(8):1115-1124. |
