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BI 639667

Cat. No. M28125
BI 639667 Structure
Synonym:

CCR1 antagonist 8

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Biological Activity

BI 639667 (compound 19n), a third azaindazole series compound, is a CCR1 antagonist, with an IC50 of 1.8 nM in Ca2+ flux assay.

Chemical Information
Molecular Weight 451.47
Formula C22H18FN5O3S
CAS Number 1295298-26-8
Form Solid
Solubility (25°C) DMSO 10 mg/mL (ultrasonic)
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] Scott V Jermain, et al. Mol Pharm. In Vitro and In Vivo Behaviors of KinetiSol and Spray-Dried Amorphous Solid Dispersions of a Weakly Basic Drug and Ionic Polymer†

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