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编 号:F427094
分子式:C21H27NO4
分子量:357.44
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
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.

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.

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.
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