[CAS NO. 928134-65-0] Osilodrostat (LCI699)

Name: Osilodrostat (LCI699)
Brand: Arctom Scientific
SKU: SLK-S7456

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PRODUCTS SPECIFICATIONS [928134-65-0]

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Catalog

SLK-S7456

Brand

Selleck

CAS

928134-65-0

DESCRIPTION [928134-65-0]

Overview

MDL	MFCD25976825
Molecular Weight	227.24
Molecular Formula	C13H10FN3
SMILES	FC1=C([C@@]2(N3C(CC2)=CN=C3)[H])C=CC(C#N)=C1

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	4.4006 mL	22.0032 mL	44.0063 mL
5 mM	0.8801 mL	4.4006 mL	8.8013 mL
10 mM	0.4401 mL	2.2003 mL	4.4006 mL
50 mM	0.0880 mL	0.4401 mL	0.8801 mL

Description

LCI699(Osilodrostat) is a potent inhibitor of , 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.

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. The administration of LCI699, up to 1.0 mg BID, effectively and safely inhibits aldosterone synthase in patients with primary aldosteronism.

References

[1] Bertagna X, et al. J Clin Endocrinol Metab. 2014, 99(4):1375-83.
[2] Amar L, et al. Hypertension. 2010 Nov;56(5):831-8.

Synonyms

Benzonitrile, 4-[(5R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl]-3-fluoro-

4-[(5R)-6,7-Dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl]-3-fluorobenzonitrile

LCI 699

Osilodrostat

4-(R)-(6,7-Dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl)-3-fluorobenzonitrile

LCI 699NX

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