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Osilodrostat (LCI699)

Cat. No. M5233
Osilodrostat (LCI699) Structure
Synonym:

Osilodrostat

Size Price Availability Quantity
5mg USD 105  USD105 In stock
10mg USD 160  USD160 In stock
25mg USD 260  USD260 In stock
50mg USD 500  USD500 In stock
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Quality Control & Documentation
Biological Activity

Osilodrostat (LCI699) is a potent inhibitor of human 11β -hydroxylase and aldosterone synthase with IC50 values of 2.5 and 0.7nM, respectively.


Chemical Information
Molecular Weight 227.24
Formula C13H10FN3
CAS Number 928134-65-0
Solubility (25°C) 45 mg/mL in DMSO
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] Li W, et al. J Chromatogr B Analyt Technol Biomed Life Sci. A semi-automated LC-MS/MS method for the determination of LCI699, a steroid 11β-hydroxylase inhibitor, in human plasma.

[2] Bertagna X J Clin Endocrinol Metab. LCI699, a potent 11β-hydroxylase inhibitor, normalizes urinary cortisol in patients with Cushing's disease: results from a multicenter, proof-of-concept study.

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Keywords: Osilodrostat (LCI699), Osilodrostat supplier, Mineralocorticoid Receptor, inhibitors, activators


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