CCR4 antagonist 3-1( —— )

Catalog No. M35402 CAS No. 1957-01-3

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Product Name

CCR4 antagonist 3-1
Note

Research use only, not for human use.
Brief Description

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.
Description

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).
In Vitro

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In Vivo

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%.
Synonyms

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Pathway

Autophagy
Target

CCR
Recptor

CCR
Research Area

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Indication

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1. Wang X, et al. Optimization of 2-aminothiazole derivatives as CCR4 antagonists. Bioorg Med Chem Lett. 2006 May 15;16(10):2800-3.?

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