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INT-767

Cat. No. M10947
INT-767  Structure
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Biological Activity

INT-767 is a farnidol X receptor (FXR)/TGR5 dual agonist,EC50 The values are 30 and 630 nM, respectively.

Chemical Information
Molecular Weight 496.68
Formula C25H45NaO6S
CAS Number 1000403-03-1
Solubility (25°C) DMSO ≥ 60 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] Kiyoaki Ito, et al. Hepatology. Dual Agonist of Farnesoid X Receptor and Takeda G Protein-Coupled Receptor 5 Inhibits Hepatitis B Virus Infection In Vitro and In Vivo

[2] Beatrice Anfuso, et al. Sci Rep. Obeticholic acid and INT-767 modulate collagen deposition in a NASH in vitro model

[3] Paolo Comeglio, et al. J Endocrinol. INT-767 prevents NASH and promotes visceral fat brown adipogenesis and mitochondrial function

[4] Jonathan D Roth, et al. World J Gastroenterol. INT-767 improves histopathological features in a diet-induced ob/ob mouse model of biopsy-confirmed non-alcoholic steatohepatitis

[5] Xiaoxin X Wang, et al. J Am Soc Nephrol. FXR/TGR5 Dual Agonist Prevents Progression of Nephropathy in Diabetes and Obesity

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