2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. Mineralocorticoid Receptor
  4. Osilodrostat phosphate

Osilodrostat phosphate  (Synonyms: LCI699 phosphate)

Cat. No.: HY-16276A Purity: 99.35%
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Osilodrostat (LCI699) phosphate is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat phosphate is a potent, orally aldosterone synthase (CYP11B2) inhibitor with IC50 values of 0.7 nM and 160 nM for human aldosterone synthase and rat aldosterone synthase, respectively. Osilodrostat phosphate inhibits aldosterone and corticosterone synthesis. Osilodrostat phosphate has blood pressure lowering ability. Osilodrostat phosphate can be used for research of Cushing syndrome (CS).

For research use only. We do not sell to patients.

Osilodrostat phosphate Chemical Structure

Osilodrostat phosphate Chemical Structure

CAS No. : 1315449-72-9

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25 mg USD 210 In-stock
50 mg USD 315 In-stock
100 mg USD 480 In-stock
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Based on 4 publication(s) in Google Scholar

Other Forms of Osilodrostat phosphate:

Osilodrostat phosphate Related Antibodies

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Description

Osilodrostat (LCI699) phosphate is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat phosphate is a potent, orally aldosterone synthase (CYP11B2) inhibitor with IC50 values of 0.7 nM and 160 nM for human aldosterone synthase and rat aldosterone synthase, respectively. Osilodrostat phosphate inhibits aldosterone and corticosterone synthesis. Osilodrostat phosphate has blood pressure lowering ability. Osilodrostat phosphate can be used for research of Cushing syndrome (CS)[1][2][3].

IC50 & Target

IC50: 35 nM (CYP11B1), 0.7 nM (human aldosterone synthase), and 160 nM (rat aldosterone synthase)[1][2]
In Vitro

Osilodrostat (LCI699; 0.01-10 µM; HAC15 cells, 17 primary human adrenocortical cell cultures, and pituitary adenoma cells) phosphate inhibits cortisol and aldosterone. Osilodrostat results in inhibition of corticosterone, 11-deoxycortisol accumulation, and modest effects on adrenal androgens[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Osilodrostat phosphate Related Antibodies
In Vivo

Osilodrostat (LCI699; 0.1-100 mg/kg; p.o.; once) phosphate inhibits aldosterone and corticosterone synthesis in Ang-II- and ACTH-stimulated Sprague Dawley rats[1].
Osilodrostat (LCI699; 3-100 mg/kg; p.o.; daily, for 52 weeks) phosphate reduces mean arterial pressure and prolongs survival in dTG rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Ang-II- and ACTH-stimulated Sprague Dawley rats[1]
Dosage: 0.1, 0.3, 1 and 3 mg/kg (Ang-II-stimulated rats) and 1, 3, 10, 30 and 100 mg/kg (ACTH-stimulated rats)
Administration: Oral administration; once
Result: Inhibited the increase in plasma aldosterone concentrations stimulated by Ang II or ACTH in a dose-dependent manner.
Animal Model: dTG rats[1]
Dosage: 3, 10, 30 and 100 mg/kg
Administration: Oral administration; daily, for 52 weeks
Result: Increased fractional LV (systolic and diastolic) shortening, normalized LV isovolumic relaxation time to RR (IVRT/RR) ratio and myocardial cell size and reduced LV weight in a dose-dependent manner.
Clinical Trial
Molecular Weight

325.23

Formula

C13H13FN3O4P
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N#CC1=CC=C([C@H]2CCC3=CN=CN32)C(F)=C1.O=P(O)(O)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : ≥ 200 mg/mL (614.95 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0747 mL 15.3737 mL 30.7475 mL
5 mM 0.6149 mL 3.0747 mL 6.1495 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

Dosing volume
(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 3.0747 mL 15.3737 mL 30.7475 mL 76.8687 mL
5 mM 0.6149 mL 3.0747 mL 6.1495 mL 15.3737 mL
10 mM 0.3075 mL 1.5374 mL 3.0747 mL 7.6869 mL
15 mM 0.2050 mL 1.0249 mL 2.0498 mL 5.1246 mL
20 mM 0.1537 mL 0.7687 mL 1.5374 mL 3.8434 mL
25 mM 0.1230 mL 0.6149 mL 1.2299 mL 3.0747 mL
30 mM 0.1025 mL 0.5125 mL 1.0249 mL 2.5623 mL
40 mM 0.0769 mL 0.3843 mL 0.7687 mL 1.9217 mL
50 mM 0.0615 mL 0.3075 mL 0.6149 mL 1.5374 mL
60 mM 0.0512 mL 0.2562 mL 0.5125 mL 1.2811 mL
80 mM 0.0384 mL 0.1922 mL 0.3843 mL 0.9609 mL
100 mM 0.0307 mL 0.1537 mL 0.3075 mL 0.7687 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Osilodrostat phosphate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Osilodrostat1315449-72-9LCI699LCI 699LCI-699Mineralocorticoid ReceptorCYP11B1Cushing syndromeblood pressureHAC15 cellsprimary human adrenocortical cell culturesInhibitorinhibitorinhibit

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