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

Osilodrostat  (Synonyms: LCI699)

Cat. No.: HY-16276 Purity: 99.90%
COA Handling Instructions

Osilodrostat (LCI699) is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat 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 inhibits aldosterone and corticosterone synthesis. Osilodrostat has blood pressure lowering ability. Osilodrostat can be used for research of Cushing syndrome (CS).

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

Osilodrostat Chemical Structure

Osilodrostat Chemical Structure

CAS No. : 928134-65-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 96 In-stock
Solution
10 mM * 1 mL in DMSO USD 96 In-stock
Solid
1 mg USD 38 In-stock
2 mg USD 55 In-stock
5 mg USD 85 In-stock
10 mg USD 130 In-stock
25 mg USD 210 In-stock
50 mg USD 315 In-stock
100 mg USD 480 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Osilodrostat:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Osilodrostat (LCI699) is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat 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 inhibits aldosterone and corticosterone synthesis. Osilodrostat has blood pressure lowering ability. Osilodrostat 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) 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.

In Vivo

Osilodrostat (LCI699; 0.1-100 mg/kg; p.o.; once) 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) 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

227.24

Formula

C13H10FN3

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (1100.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 100 mg/mL (440.06 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent 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
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (11.00 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (11.00 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.90%

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 4.4006 mL 22.0032 mL 44.0063 mL 110.0158 mL
5 mM 0.8801 mL 4.4006 mL 8.8013 mL 22.0032 mL
10 mM 0.4401 mL 2.2003 mL 4.4006 mL 11.0016 mL
15 mM 0.2934 mL 1.4669 mL 2.9338 mL 7.3344 mL
20 mM 0.2200 mL 1.1002 mL 2.2003 mL 5.5008 mL
25 mM 0.1760 mL 0.8801 mL 1.7603 mL 4.4006 mL
30 mM 0.1467 mL 0.7334 mL 1.4669 mL 3.6672 mL
40 mM 0.1100 mL 0.5501 mL 1.1002 mL 2.7504 mL
50 mM 0.0880 mL 0.4401 mL 0.8801 mL 2.2003 mL
60 mM 0.0733 mL 0.3667 mL 0.7334 mL 1.8336 mL
80 mM 0.0550 mL 0.2750 mL 0.5501 mL 1.3752 mL
100 mM 0.0440 mL 0.2200 mL 0.4401 mL 1.1002 mL
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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.

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Osilodrostat
Cat. No.:
HY-16276
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