CCR4 antagonist 3-1

Research use only, not for human use.

CCR4 antagonist 3-1 is a less active chemokine receptor 4 (CCR4) antagonist that inhibits [125I]TARC (thymus and activation-regulated chemokine) with an IC50 value of 1.7 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 : 62.5 mg/mL (260.07 mM; Ultrasonic )

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

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(-20℃)

With Ice Pack

≥ 2 years