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BMS-986339

Cat. No. M21058
BMS-986339  Structure
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Biological Activity

BMS-986339 is an oral farnesoid X receptor (FXR) agonist being developed for nonalcoholic steatohepatitis (NASH).

Chemical Information
Molecular Weight 643.71
Formula C35H41F4N3O4
CAS Number 2477873-64-4
Solubility (25°C) N/A
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] Susheel J Nara, et al. J Med Chem. Discovery of BMS-986339, a Pharmacologically Differentiated Farnesoid X Receptor Agonist for the Treatment of Nonalcoholic Steatohepatitis

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Keywords: BMS-986339 supplier, Farnesoid X Receptor, inhibitors, activators


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