DY268 is a potent FXR antagonist with IC50 of 7.5 nM. DY 268 exhibits no detectable cytotoxicity in cell-based assays.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 40 mg/mL|
Identification of trisubstituted-pyrazol carboxamide analogs as novel and potent antagonists of farnesoid X receptor.
Yu DD, et al. Bioorg Med Chem. 2014 Jun 1;22(11):2919-38. PMID: 24775917.
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