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BMS-817399 

Cat. No. M27929
BMS-817399  Structure
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Biological Activity

BMS-817399 is a potent, selective, and orally bioavailable CCR1 antagonist. BMS-817399 exhibits CCR1 binding affinity and chemotaxis inhibition potencies of 1 and 6 nM (IC50), respectively. BMS-817399 can be used for the research of rheumatoid arthritis.

Chemical Information
Molecular Weight 454
Formula C23H36ClN3O4
CAS Number 1202400-18-7
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Jun Shu, et al. Front Aging Neurosci. Identification of potential drυg targets for vascular dementia and carotid plaques by analyzing underlying molecular signatures shared by them

[2] Bonnie Wang, et al. AAPS J. Investigation on the Effect of Capillary Microsampling on Hematologic and Toxicokinetic Evaluation in Regulatory Safety Studies in Mice

[3] Huijun Chen, et al. J Pharm Sci. Moisture-Induced Amorphous Phase Separation of Amorphous Solid Dispersions: Molecular Mechanism, Microstructure, and Its Impact on Dissolution Performance

[4] Javed A Khan, et al. J Mol Biol. Developing Adnectins that target SRC co-activator binding to PXR: a structural approach toward understanding promiscuity of PXR

[5] Joseph B Santella 3rd, et al. J Med Chem. Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis

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Keywords: BMS-817399  supplier, CCR, inhibitors, activators

 
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