Home Metabolism Hydroxylase inhibitor - P450 (e.g. CYP17) inhibitor Osilodrostat (LCI699) For research use only.

Osilodrostat (LCI699)

LCI699(Osilodrostat) is a potent inhibitor of 11β-hydroxylase (CYP11B), an enzyme catalyzing the final step of cortisol synthesis.

Osilodrostat (LCI699) Chemical Structure

Osilodrostat (LCI699) Chemical Structure

CAS No. 928134-65-0

Purity & Quality Control

Batch: S745601 DMSO]45 mg/mL]false]Ethanol]45 mg/mL]false]Water]Insoluble]false Purity: 99.98%
99.98

Osilodrostat (LCI699) Related Products

Signaling Pathway

Hydroxylase Signaling Pathways

Hydroxylase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
V79MZh cells Function assay Inhibition of human CYP11B2 expressed in hamster V79MZh cells using deoxycorticosterone as substrate, IC50=0.2 nM 24899257
NCI-H295R cells Function assay Inhibition of CYP11B2 in human NCI-H295R cells assessed as inhibition of angiotensin-2-induced aldosterone production after 24 hrs by RIA, IC50=9 nM 24900631
renal leiomyoblastoma cells Function assay Inhibition of mouse CYP11B2 expressed in renal leiomyoblastoma cells, IC50=0.21 μM 26403853
Click to View More Cell Line Experimental Data

Biological Activity

Description LCI699(Osilodrostat) is a potent inhibitor of 11β-hydroxylase (CYP11B), an enzyme catalyzing the final step of cortisol synthesis.
Targets
11β-hydroxylase [1]
2.5 nM
In vitro
In vitro LCI699 also inhibits aldosterone synthase (CYP11B2) other than CYP11B1[1].
In Vivo
In vivo LCI699 is a potent inhibitor of 11β-hydroxylase (CYP11B1), the enzyme that catalyzes the final step of cortisol synthesis, and has a half-life of ∼4 hours. It decreases blood pressure (BP) in patients with essential hypertension and primary aldosteronism. Treatment with LCI699 is well tolerated, it is demonstrated efficacy with a satisfactory safety and tolerability profile in the proof-of-concept study in Cushing's disease[1]. The administration of LCI699, up to 1.0 mg BID, effectively and safely inhibits aldosterone synthase in patients with primary aldosteronism[2].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05382156 Recruiting
Endogenous Cushing''s Syndrome
RECORDATI GROUP
 June 13 2022 --
NCT03708900 Unknown status
Cushing''s Disease
RECORDATI GROUP
 April 28 2021 Phase 2
NCT02697734 Completed
Cushing''s Disease
Novartis Pharmaceuticals|Novartis
 October 3 2016 Phase 3
NCT02399202 Completed
Renal Impairment
Novartis Pharmaceuticals|Novartis
 November 6 2015 Phase 1
NCT02468193 Completed
Cushing''s Syndrome|Ectopic Corticotropin Syndrome|Adrenal Adenoma|Adrenal Carcinoma|AIMAH|PPNAD
Novartis Pharmaceuticals|Novartis
 September 24 2015 Phase 2
NCT02372084 Completed
Hepatic Impairment
Novartis Pharmaceuticals|Novartis
 April 21 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 227.24 Formula

C13H10FN3
CAS No. 928134-65-0 SDF Download Osilodrostat (LCI699) SDF
Smiles C1CC2=CN=CN2C1C3=C(C=C(C=C3)C#N)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 45 mg/mL ( (198.02 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 45 mg/mL

Water : Insoluble


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In vivo
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In vivo Formulation Calculator

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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