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.
IC50&Target
CCR8
体外研究
R243 has CCR8-antagonistic effects on CCL1-induced Ca2+ flux and CCL1-driven peritoneal macrophages aggregation.
R243 attenuates secretion of TNF-α, IL-6, and most strikingly IL-10 from wild-type peritoneal macrophages (WT PMφ).
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.
体内研究
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.
Animal Model:
Male Swiss mice (7-9 weeks old) injected with CCL1
Dosage:
0.1 mg/kg, 0.3mg/kg, 1 mg/kg
Administration:
Intraperitoneal injection; once
Result:
The analgesic effect evoked by CCL1 (10 μg/kg; 1 h; s.c.) was dose-dependently inhibited.
分子式
C21H27NO4
分子量
357.44
CAS号
688352-84-3
运输条件
Room temperature in continental US; may vary elsewhere.