| Bioactivity | ML604086 is a selective CCR8 inhibitor, inhibiting CCL1 binding to CCR8 on circulating T-cells. ML604086 inhibits CCL1 mediated chemotaxis and increases in intracellular Ca2+ concentrations[1][2]. | ||||||||||||
| Target | CCR8. | ||||||||||||
| Invitro | ML604086 (0-100 µM) inhibits CCL1 mediated chemotaxis and increases in intracellular Ca2+ concentrations of cell lines stably expressing cyno CCR8 with IC50s of 1.3 µM and 1.0 µM, respectively[2].ML604086 (10, 30 µM; 64 h) inhibits CCL1 binding to CCR8 on CD4 T-cells, and inhibits the serotonin receptor 5HT1a with the inhibition rate of 30%, 70% at 10, 30 µM respectively[2]. | ||||||||||||
| In Vivo | ML604086 (1.038 mg/kg; intravenous infusion) shows no effect on airway eosinophilia, pro-inflammatory cytokine production or airway resistance and compliance in Macaca fascicularis[1]. Animal Model: | ||||||||||||
| Name | ML604086 | ||||||||||||
| CAS | 850330-18-6 | ||||||||||||
| Formula | C27H32N4O4S | ||||||||||||
| Molar Mass | 508.63 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. James E. Pease, et al. Chemokine Receptors in Allergy, Inflammation, and Infectious Disease. Top Med Chem (2015) 14: 1-40. [2]. Lin Wang, et al. Antagonism of chemokine receptor CCR8 is ineffective in a primate model of asthma. Thorax 2013;68:506–512. |
ML604086
CAS: 850330-18-6 F: C27H32N4O4S W: 508.63
ML604086 is a selective CCR8 inhibitor, inhibiting CCL1 binding to CCR8 on circulating T-cells. ML604086 inhibits CCL1 m
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