Osilodrostat

Modify Date: 2024-01-06 14:13:47

Osilodrostat Structure
Osilodrostat structure
 Common Name Osilodrostat
CAS Number 928134-65-0 Molecular Weight 227.237
Density 1.3±0.1 g/cm3 Boiling Point 433.8±45.0 °C at 760 mmHg
Molecular Formula C13H10FN3 Melting Point N/A
MSDS N/A Flash Point 216.2±28.7 °C

 Use of Osilodrostat


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

 Names

Name 4-[(5R)-6,7-Dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl]-3-fluorobenzo nitrile
Synonym More Synonyms

 Osilodrostat Biological Activity

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

IC50: 2.5 nM (human 11β-hydroxylase), 0.7 nM (aldosterone synthase)[1]
In Vivo Osilodrostat and pasireotide monotherapies are associated with significant changes in the histology and mean weights of the pituitary and adrenal glands, liver, and ovary/oviduct. Osilodrostat alone is associated with adrenocortical hypertrophy and hepatocellular hypertrophy. In combination, osilodrostat/pasireotide does not exacerbate any target organ changes and ameliorated the liver and adrenal gland changes observed with monotherapy. Cmax and AUC0–24h of osilodrostat and pasireotide increase in an approximately dose-proportional manner[1]. Osilodrostat treatment reduces urinary free cortisol in patients with Cushing's disease; 78.9% has normal urinary free cortisol at week 22. Treatment with osilodrostat is generally well tolerated[2].
Animal Admin Rats: Sixty male and 60 female rats are randomized into single-sex groups to receive daily doses of pasireotide (0.3 mg/kg/day, subcutaneously), osilodrostat (20 mg/kg/day, orally), osilodrostat/pasireotide in combination (low dose, 1.5/0.03 mg/kg/day; mid-dose, 5/0.1 mg/kg/day; or high dose, 20/0.3 mg/kg/day), or vehicle for 13 weeks[1].
References

[1]. Li L, et al. Osilodrostat (LCI699), a potent 11β-hydroxylase inhibitor, administered in combination with the multireceptor-targeted somatostatin analog pasireotide: A 13-week study in rats. Toxicol Appl Pharmacol. 2015 Aug 1;286(3):224-33.

[2]. Fleseriu M, et al. Osilodrostat, a potent oral 11β-hydroxylase inhibitor: 22-week, prospective, Phase II study in Cushing's disease. Pituitary. 2016 Apr;19(2):138-48.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 433.8±45.0 °C at 760 mmHg
Molecular Formula C13H10FN3
Molecular Weight 227.237
Flash Point 216.2±28.7 °C
Exact Mass 227.085876
PSA 41.61000
LogP 1.13
Vapour Pressure 0.0±1.0 mmHg at 25°C
Index of Refraction 1.664
Storage condition -20℃

 Synthetic Route

2-Fluoro-4-Cyanobenzyl Bromide structure

2-Fluoro-4-Cyan...

CAS#:105942-09-4

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Osilodrostat Structure

Osilodrostat

CAS#:928134-65-0

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CAS#:928134-66-1
Literature: Meredith, Erik L.; Ksander, Gary; Monovich, Lauren G.; Papillon, Julien P. N.; Liu, Qian; Miranda, Karl; Morris, Patrick; Rao, Chang; Burgis, Robin; Capparelli, Michael; Hu, Qi-Ying; Singh, Alok; Rigel, Dean F.; Jeng, Arco Y.; Beil, Michael; Fu, Fumin; Hu, Chii-Whei; Lasala, Daniel ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 12 p. 1203 - 1207
3-Fluoro-4-methylbenzonitrile structure

3-Fluoro-4-meth...

CAS#:170572-49-3

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Osilodrostat Structure

Osilodrostat

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N/A structure

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CAS#:928134-66-1
Literature: Meredith, Erik L.; Ksander, Gary; Monovich, Lauren G.; Papillon, Julien P. N.; Liu, Qian; Miranda, Karl; Morris, Patrick; Rao, Chang; Burgis, Robin; Capparelli, Michael; Hu, Qi-Ying; Singh, Alok; Rigel, Dean F.; Jeng, Arco Y.; Beil, Michael; Fu, Fumin; Hu, Chii-Whei; Lasala, Daniel ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 12 p. 1203 - 1207
2-(1-tritylimidazol-4-yl)acetic acid structure

2-(1-tritylimid...

CAS#:168632-03-9

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Osilodrostat Structure

Osilodrostat

CAS#:928134-65-0

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CAS#:928134-66-1
Literature: Meredith, Erik L.; Ksander, Gary; Monovich, Lauren G.; Papillon, Julien P. N.; Liu, Qian; Miranda, Karl; Morris, Patrick; Rao, Chang; Burgis, Robin; Capparelli, Michael; Hu, Qi-Ying; Singh, Alok; Rigel, Dean F.; Jeng, Arco Y.; Beil, Michael; Fu, Fumin; Hu, Chii-Whei; Lasala, Daniel ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 12 p. 1203 - 1207
1H-Imidazole, 4-[2-[[(1,1-dimethylethyl)dimethylsilyl]oxy]ethyl]-1-(triphenylmethyl) structure

1H-Imidazole, 4...

CAS#:928136-82-7

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Osilodrostat Structure

Osilodrostat

CAS#:928134-65-0

N/A structure

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CAS#:928134-66-1
Literature: Meredith, Erik L.; Ksander, Gary; Monovich, Lauren G.; Papillon, Julien P. N.; Liu, Qian; Miranda, Karl; Morris, Patrick; Rao, Chang; Burgis, Robin; Capparelli, Michael; Hu, Qi-Ying; Singh, Alok; Rigel, Dean F.; Jeng, Arco Y.; Beil, Michael; Fu, Fumin; Hu, Chii-Whei; Lasala, Daniel ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 12 p. 1203 - 1207
N/A structure

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CAS#:1472004-27-5

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Osilodrostat Structure

Osilodrostat

CAS#:928134-65-0

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CAS#:928134-66-1
Literature: Meredith, Erik L.; Ksander, Gary; Monovich, Lauren G.; Papillon, Julien P. N.; Liu, Qian; Miranda, Karl; Morris, Patrick; Rao, Chang; Burgis, Robin; Capparelli, Michael; Hu, Qi-Ying; Singh, Alok; Rigel, Dean F.; Jeng, Arco Y.; Beil, Michael; Fu, Fumin; Hu, Chii-Whei; Lasala, Daniel ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 12 p. 1203 - 1207
methyl 2-(4-cyano-2-fluorophenyl)-2-(5-(2-((methylsulfonyl)oxy)ethyl)-1H-imidazol-1-yl)acetate structure

methyl 2-(4-cya...

CAS#:1472004-21-9

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Osilodrostat Structure

Osilodrostat

CAS#:928134-65-0

N/A structure

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CAS#:928134-66-1
Literature: Meredith, Erik L.; Ksander, Gary; Monovich, Lauren G.; Papillon, Julien P. N.; Liu, Qian; Miranda, Karl; Morris, Patrick; Rao, Chang; Burgis, Robin; Capparelli, Michael; Hu, Qi-Ying; Singh, Alok; Rigel, Dean F.; Jeng, Arco Y.; Beil, Michael; Fu, Fumin; Hu, Chii-Whei; Lasala, Daniel ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 12 p. 1203 - 1207
4-((5-(2-((tert-butyldimethylsilanyl)oxy)ethyl)-1H-imidazol-1-yl)methyl)-3-fluorobenzonitrile structure

4-((5-(2-((tert...

CAS#:1472004-15-1

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Osilodrostat Structure

Osilodrostat

CAS#:928134-65-0

N/A structure

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CAS#:928134-66-1
Literature: Meredith, Erik L.; Ksander, Gary; Monovich, Lauren G.; Papillon, Julien P. N.; Liu, Qian; Miranda, Karl; Morris, Patrick; Rao, Chang; Burgis, Robin; Capparelli, Michael; Hu, Qi-Ying; Singh, Alok; Rigel, Dean F.; Jeng, Arco Y.; Beil, Michael; Fu, Fumin; Hu, Chii-Whei; Lasala, Daniel ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 12 p. 1203 - 1207
methyl 2-(5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1H-imidazol-1-yl)-2-(4-cyano-2-fluorophenyl)acetate structure

methyl 2-(5-(2-...

CAS#:1567653-71-7

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Osilodrostat Structure

Osilodrostat

CAS#:928134-65-0

N/A structure

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CAS#:928134-66-1
Literature: Meredith, Erik L.; Ksander, Gary; Monovich, Lauren G.; Papillon, Julien P. N.; Liu, Qian; Miranda, Karl; Morris, Patrick; Rao, Chang; Burgis, Robin; Capparelli, Michael; Hu, Qi-Ying; Singh, Alok; Rigel, Dean F.; Jeng, Arco Y.; Beil, Michael; Fu, Fumin; Hu, Chii-Whei; Lasala, Daniel ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 12 p. 1203 - 1207
N/A structure

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CAS#:928134-37-6

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Osilodrostat Structure

Osilodrostat

CAS#:928134-65-0

N/A structure

N/A

CAS#:928134-66-1
Literature: Meredith, Erik L.; Ksander, Gary; Monovich, Lauren G.; Papillon, Julien P. N.; Liu, Qian; Miranda, Karl; Morris, Patrick; Rao, Chang; Burgis, Robin; Capparelli, Michael; Hu, Qi-Ying; Singh, Alok; Rigel, Dean F.; Jeng, Arco Y.; Beil, Michael; Fu, Fumin; Hu, Chii-Whei; Lasala, Daniel ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 12 p. 1203 - 1207

 Synonyms

osilodrostat
4-(quinolin-3-ylmethyl-amino)-benzenesulfonamide
Novartis LCI699
(R)-4-(6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl)-3-fluorobenzonitrile
UNII-5YL4IQ1078
4-[(5R)-6,7-Dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl]-3-fluorobenzonitrile
Benzonitrile, 4-[(5R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl]-3-fluoro-
3-<N-(4'-Amidosulfonylphenyl)aminomethyl>quinoline
4-((R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl)-3-fluoro-benzonitrile
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Related Compounds: More...
osilodrostat phosphate
1315449-72-9
Chemsrc provides Osilodrostat(CAS#:928134-65-0) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of Osilodrostat are included as well.>> amp version: Osilodrostat

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