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CCX354 

Cat. No. M27628
CCX354  Structure
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Biological Activity

CCX354 is an antagonist of CCR1, with anti-inflammatory activity.

Chemical Information
Molecular Weight 451.91
Formula C22H22ClN7O2
CAS Number 1010073-75-2
Form Solid
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] A Gilchrist, et al. Br J Pharmacol. Identifying bias in CCR1 antagonists using radiolabelled binding, receptor internalization, β-arrestin translocation and chemotaxis assays

[2] Daniel J Dairaghi, et al. Blood. CCR1 blockade reduces tumor burden and osteolysis in vivo in a mouse model of myeloma bone disease

[3] Paul P Tak, et al. Ann Rheum Dis. Chemokine receptor CCR1 antagonist CCX354-C treatment for rheumatoid arthritis: CARAT-2, a randomised, placebo controlled clinical trial

[4] Roy Fleischmann. Curr Opin Rheumatol. Novel small-molecular therapeutics for rheumatoid arthritis

[5] D J Dairaghi, et al. Clin Pharmacol Ther. Pharmacokinetic and pharmacodynamic evaluation of the novel CCR1 antagonist CCX354 in healthy human subjects: implications for selection of clinical dose

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Keywords: CCX354  supplier, CCR, inhibitors, activators


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