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CCR7 antagonist 1

Cat. No. M41798
CCR7 antagonist 1 Structure
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Biological Activity

CCR7 antagonist 1 is a dual CXCR2 (IC50 of 11.02 μM) and CCR7 (IC50 of 0.43 μM) antagonist.

Chemical Information
Molecular Weight 310.42
Formula C13H22N6OS
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Kristoffer H Johansen et al. Front Immunol. PI3K in T Cell Adhesion and Trafficking

[2] Anwar Salem et al. Biochim Biophys Acta Rev Cancer. CCR7 as a therapeutic target in Cancer

[3] Barbara Maier et al. Nature. A conserved dendritic-cell regulatory program limits antitumour immunity

[4] Shirsha Saha et al. Biochemistry. The Inside Story: Crystal Structure of the Chemokine Receptor CCR7 with an Intracellular Allosteric Antagonist

[5] Haruko Hayasaka et al. PLoS One. The HIV-1 Gp120/CXCR4 axis promotes CCR7 ligand-dependent CD4 T cell migration: CCR7 homo- and CCR7/CXCR4 hetero-oligomer formation as a possible mechanism for up-regulation of functional CCR7

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