| Bioactivity | 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]. |
| 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: |
| Name | CCR4 antagonist 3-1 |
| CAS | 1957-01-3 |
| Formula | C14H12N2S |
| Molar Mass | 240.32 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Wang X, et al. Optimization of 2-aminothiazole derivatives as CCR4 antagonists. Bioorg Med Chem Lett. 2006 May 15;16(10):2800-3. |