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Osilodrostat phosphate

Cat. No. M28169
Osilodrostat phosphate Structure
Synonym:

LCI699 phosphate

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Biological Activity

Osilodrostat (LCI699) phosphate is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat phosphate is a potent, orally aldosterone synthase (CYP11B2) inhibitor with IC50 values of 0.7 nM and 160 nM for human aldosterone synthase and rat aldosterone synthase, respectively. Osilodrostat phosphate inhibits aldosterone and corticosterone synthesis. Osilodrostat phosphate has blood pressure lowering ability. Osilodrostat phosphate can be used for research of Cushing syndrome (CS).

Chemical Information
Molecular Weight 325.23
Formula C13H13FN3O4P
CAS Number 1315449-72-9
Form Solid
Solubility (25°C) Water ≥ 120 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] No authors listed. Osilodrostat

[2] Nancy J Brown. Nat Rev Nephrol. Contribution of aldosterone to cardiovascular and renal inflammation and fibrosis

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Keywords: Osilodrostat phosphate, LCI699 phosphate supplier, Mineralocorticoid Receptor, inhibitors, activators


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