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BMS-823778

Cat. No. M7671
BMS-823778 Structure
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Biological Activity

BMS-823778 is an orally available potent and selective inhibitor of 11-β-hydroxysteroid-dehydrogenase 1 (11βHSD-1). BMS-823778 is an antihyperglycaemic.

Chemical Information
Molecular Weight 364.27
Formula C18H18ClN3O · HCl
CAS Number 1140898-87-8
Solubility (25°C) DMSO: 5 mg/mL
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] Jun Li, et al. Discovery of Clinical Candidate BMS-823778 as an Inhibitor of Human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD-1)

[2] Jiachang Gong, et al. Physiologically-based pharmacokinetic modelling of a CYP2C19 substrate, BMS-823778, utilizing pharmacogenetic data

[3] Jiachang Gong, et al. Clinical Pharmacokinetics and the Impact of Genetic Polymorphism on a CYP2C19 Substrate, BMS-823778, in Healthy Subjects

[4] Yaofeng Cheng, et al. Clinical significance of CYP2C19 polymorphisms on the metabolism and pharmacokinetics of 11β-hydroxysteroid dehydrogenase type-1 inhibitor BMS-823778

[5] Brad D Maxwell, et al. The syntheses of [(14) C]BMS-823778 for use in a human ADME clinical study and of [(13) CD3 (13) CD2 ]BMT-094817, a stable-isotope labeled standard of a newly detected human metabolite

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Keywords: BMS-823778 supplier, Hydroxysteroid dehydrogenase, inhibitors, activators


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