CCR4 antagonist 3-1

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

CCR4 antagonist 3 是一种有效的趋化因子受体 4 (CCR4) 拮抗剂，对 [125I]TARC (胸腺和活化调节趋化因子) 的 IC50 为 1.7 μM。CCR4 antagonist 3 可抑制 CEM 细胞表面 [125I]TARC和巨噬细胞来源的趋化因子 (MDC) 与 CCR4 受体的结合。CCR4 antagonist 3 也能在体外抑制 TARC 介导的 CEM 细胞迁移 (IC50=6.4 μM)。

CCR4 antagonist 3 is a potent chemokine receptor 4 (CCR4) antagonist with an IC50 value of 1.7 μM for [125I]TARC (thymus and activation regulated chemokine). CCR4 antagonist 3 inhibits binding of radiolabeled TARC and macrophage-derived chemokine (MDC) to CCR4 receptors on the surface of CEM cells. CCR4 antagonist 3 also inhibits the in vitro migration of CEM cells mediated by TARC (IC50 = 6.4 μM).

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CCR4 antagonist 3 (compound 1) (0.5 mg/kg for IV; 2 mg/kg for PO; single dosage) exhibits a high clearance, short half-life and low oral bioavailability.Animal Model:Rats Dosage:0.5 mg/kg for IV; 2 mg/kg for PO Administration:IV and PO; single dosage Result:Exhibited a high clearance of 4.2 L/h/kg and a short half-life of 0.4 h, and the oral bioavailability of 2%.

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Autophagy

CCR

CCR

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1957-01-3

240.32

C14H12N2S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 62.5 mg/mL (260.07 mM; 超声助溶 )

N(C=1C2=C(C=CC1)C=CC=C2)C3=NC(C)=CS3

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(-20℃)

With Ice Pack

≥ 2 years