R243

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

R243 是一种有效的小分子 CCR8 拮抗剂，可抑制 CCR8 信号传导和趋化性。

R243 is a potent, small molecule CCR8 antagonist that inhibits CCR8 signaling and chemotaxis, inhibits CCL1-induced Ca2+ flux and CCL1-driven peritoneal macrophages aggregation at 0.2 uM; attenuated secretion of TNF-α, IL-6, and most strikingly IL-10 from WT PMφ (peritoneal macrophages), but not BMMφ (bone marrow-derived macrophages); shows suppressed c-JNK activity and NF-κB signaling after LPS treatment, suppresses LPS-induced cytokine secretion; attenuates peritoneal adhesions in vivo in CCR8-/- mice, also prevents hapten-induced colitis.

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.

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.

R-243 | R 243

GPCR/G Protein

Chemokine Receptor

Chemokine Receptor

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688352-84-3

357.45

C21H27NO4

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (349.71 mM)

N1(CCOC2(C3)CC4CC3CC(C4)C2)COC5=CC(OCO6)=C6C=C5C1

7,8-Dihydro-7-[2-(tricyclo[3.3.1.1(3,7)]dec-1-yloxy)ethyl]-6H-1,3-dioxolo[4,5-g][1,3]benzoxazine

(-20℃)

With Ice Pack

≥ 2 years