Osilodrostat (LCI699)

Catalog No.S7456 Synonyms: Osilodrostat

Osilodrostat (LCI699) Chemical Structure

Molecular Weight(MW): 227.24

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

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Biological Activity

Description LCI699(Osilodrostat) is a potent inhibitor of 11β-hydroxylase, 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 MoPaSpVv[3Srb36gZZN{[Xl? MYPJcohq[mm2aX;uJI9nKGi3bXHuJGN[WDFzQkKg[ZhxemW|c3XkJIlvKGijbYP0[ZIhXjd7TWroJINmdGy|IIXzbY5oKGSnb4j5Z49zfGmlb4P0[ZJwdmViYYOgd5Vje3S{YYTlMEBKSzVyPUCuNkBvVQ>? MoHmNlQ5QTl{NUe=
NCI-H295R cells NIPTRY1HfW6ldHnvckBie3OjeR?= NWr3NFZPUW6qaXLpeIlwdiCxZjDDXXAyOUJ{IHnuJIh2dWGwIF7DTU1JOjl3UjDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGGwZ3nveIVve2mwLUKtbY5lfWOnZDDhcIRwe3Sncn;u[UBxem:mdXP0bY9vKGGodHXyJFI1KGi{czDifUBTUUFuIFnDOVA:QSCwTR?= M1;IUlI1QTByNkOx
renal leiomyoblastoma cells NWT4Tm5DTnWwY4Tpc44h[XO|YYm= MonTTY5pcWKrdHnvckBw\iCvb4Xz[UBEYVBzMVKyJIV5eHKnc4Pl[EBqdiC{ZX7hcEBt\WmxbYnvZoxie3SxbXGgZ4VtdHNuIFnDOVA:OC5{MTFOwG0> MWqyOlQxOzh3Mx?=

... Click to View More Cell Line Experimental Data

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

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 227.24
Formula

C13H10FN3

CAS No. 928134-65-0
Storage powder
in solvent
Synonyms Osilodrostat

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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 31 2019 Phase 2
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 Active not recruiting Drug: LCI699|Drug: LCI699 matching placebo Cushing''s Disease Novartis Pharmaceuticals|Novartis October 6 2014 Phase 3
NCT01331239 Active not recruiting Drug: LCI699 Cushing''s Disease Novartis Pharmaceuticals|Novartis March 23 2011 Phase 2

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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.

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Hydroxylase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID