LMD-009

LMD-009 is a selective CCR8 nonpeptide agonist. LMD-009 mediates chemotaxis, inositol phosphate accumulation, and calcium release in high potencies with EC 50 s from 11 to 87 nM In Vitro LMD-009 (0-20 nM; 90 min) stimulates inositol phosphate accumulation in COS-7 cells expressing the human CCR8 receptor. LMD-009 (0-100 nM; 1 h) mediates calcium release in Chinese hamster ovary cells. LMD-009 (0.1 nM-100 μM; 40 min) induces L1.2 cells migration. LMD-009 (0-10 μM; 90 min) exhibits different molecular interaction with CCR8 mutations in COS-7 cells. LMD-009 (0-10 nM; 90 min) exhibits no antagonist activity to other human chemokine receptors. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: COS-7 cells Concentration: 0-20 nM Incubation Time: 90 min Result: Stimulated inositol phosphate accumulation in COS-7 cells expressing the human CCR8 receptor with an EC 50 value of 11 nM. Inhibited none of the receptors of other human chemokine receptors. Cell Viability AssayCell Line: Chinese hamster ovary cells Concentration: 0-100 nM Incubation Time: 1 hour Result: Regulated calcium release in Chinese hamster ovary cells with an EC 50 value 87 nM. Cell Migration AssayCell Line: Lymphocyte L1.2 cells. Concentration: 0.1 nM- 100 μM Incubation Time: 40 min Result: Exhibited an K i value of 66 nM with L1.2 cells and specifically bound 125 I-CCL1. Form:Solid IC50& Target:CCR8 11-87 nM (EC 50 )

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