Osilodrostat (LCI699)

Catalog No.S7456

For research use only.

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

Osilodrostat (LCI699) Chemical Structure

CAS No. 928134-65-0

Selleck's Osilodrostat (LCI699) has been cited by 2 Publications

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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

LCI699 also inhibits aldosterone synthase (CYP11B2) other than CYP11B1[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
V79MZh cells NVX1dpZFTnWwY4Tpc44h[XO|YYm= NVzUT5lKUW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIzKGW6cILld5Nm\CCrbjDoZY1{fGW{IG[3PW1bcCClZXzsd{B2e2mwZzDk[Y95gWOxcoTpZ49{fGW{b37lJIF{KHO3YoP0doF1\SxiSVO1NF0xNjJibl2= MYeyOFg6QTJ3Nx?=
NCI-H295R cells NHHyT2tHfW6ldHnvckBie3OjeR?= NUjBW3VOUW6qaXLpeIlwdiCxZjDDXXAyOUJ{IHnuJIh2dWGwIF7DTU1JOjl3UjDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGGwZ3nveIVve2mwLUKtbY5lfWOnZDDhcIRwe3Sncn;u[UBxem:mdXP0bY9vKGGodHXyJFI1KGi{czDifUBTUUFuIFnDOVA:QSCwTR?= M1LtWlI1QTByNkOx
renal leiomyoblastoma cells M2rBUGZ2dmO2aX;uJIF{e2G7 NVjhZZVZUW6qaXLpeIlwdiCxZjDtc5V{\SCFWWCxNWIzKGW6cILld5Nm\CCrbjDy[Y5idCCuZXnvcZlw[myjc4TvcYEh[2WubIOsJGlEPTB;MD6yNUDPxE1? NG\lTFMzPjRyM{i1Ny=>
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].

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 45 mg/mL
(198.02 mM)
Water 15 mg/mL
(66.0 mM)
Ethanol '45 mg/mL

Chemical Information

Molecular Weight 227.24
Formula

C13H10FN3

CAS No. 928134-65-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC2=CN=CN2C1C3=C(C=C(C=C3)C#N)F

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03708900 Recruiting Drug: LCI699 Cushing''s Disease Novartis Pharmaceuticals|Novartis October 30 2020 Phase 2
NCT02697734 Completed Drug: osilodrostat|Drug: osilodrostat Placebo Cushing''s Disease Novartis Pharmaceuticals|Novartis October 3 2016 Phase 3
NCT02399202 Completed Drug: osilodrostat Renal Impairment Novartis Pharmaceuticals|Novartis November 6 2015 Phase 1
NCT02468193 Completed Drug: Osilodrostat Cushing''s Syndrome|Ectopic Corticotropin Syndrome|Adrenal Adenoma|Adrenal Carcinoma|AIMAH|PPNAD Novartis Pharmaceuticals|Novartis September 24 2015 Phase 2
NCT02372084 Completed Drug: osilodrostat Hepatic Impairment Novartis Pharmaceuticals|Novartis April 21 2015 Phase 1
NCT02180217 Completed Drug: osilodrostat|Drug: LCI699 matching placebo Cushings Disease Novartis Pharmaceuticals|Novartis October 6 2014 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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