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FR194738

Cat. No. M15106
FR194738  Structure
Size Price Availability Quantity
5mg USD 595  USD595 In stock
10mg USD 1020  USD1020 In stock
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Quality Control & Documentation
Biological Activity

FR194738 inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM. FR194738 is a squalene epoxidase inhibitor.

Chemical Information
Molecular Weight 476.12
Formula C27H38ClNO2S
CAS Number 204067-52-7
Solubility (25°C) DMSO ≥ 200 mg/mL
Storage 4°C, dry, sealed
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] Xun Shangguan, et al. Cancer Res. Squalene epoxidase metabolic dependency is a targetable vulnerability in castration-resistant prostate cancer

[2] Masae Sawada, et al. Bioorg Med Chem Lett. Synthesis and biological activity of a novel squalene epoxidase inhibitor, FR194738

[3] Masae Sawada, et al. Biol Pharm Bull. Inhibition of cholesterol synthesis causes both hypercholesterolemia and hypocholesterolemia in hamsters

[4] M Sawada, et al. Eur J Pharmacol. Effect of FR194738, a potent inhibitor of squalene epoxidase, on cholesterol metabolism in HepG2 cells

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