CCR4 antagonist 3-1

Names

[ CAS No. ]:
1957-01-3

[ Name ]:
CCR4 antagonist 3-1

Biological Activity

[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)[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> CCR
Signaling Pathways >> Immunology/Inflammation >> CCR
Research Areas >> Inflammation/Immunology

[Target]

CCR4

[125I]-TARC-CCR4:1.7 μM (IC50)


[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[1]. Animal Model: Rats[1] 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%.

[References]

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

Chemical & Physical Properties

[ Molecular Formula ]:
C14H12N2S

[ Molecular Weight ]:
240.32

Related Compounds