| 规格: | 98% |
| 分子量: | 357.44 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
Background:
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].
[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.
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