1. Immunology/Inflammation Vitamin D Related/Nuclear Receptor Apoptosis
  2. Glucocorticoid Receptor Apoptosis Caspase
  3. Nenocorilant

Nenocorilantis a potent, orally activity glucocorticoid receptor (GR) antagonist with Ki value of 0.15 nM. Nenocorilant has pro-apoptotic effects and improves potency combined with cytotoxic agent. Nenocorilant can be used for cancer research.

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

Nenocorilant Chemical Structure

Nenocorilant Chemical Structure

CAS No. : 1496509-78-4

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5 mg USD 580 In-stock
10 mg USD 930 In-stock
25 mg USD 1860 In-stock
50 mg USD 3000 In-stock
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200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Nenocorilant

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Nenocorilantis a potent, orally activity glucocorticoid receptor (GR) antagonist with Ki value of 0.15 nM. Nenocorilant has pro-apoptotic effects and improves potency combined with cytotoxic agent. Nenocorilant can be used for cancer research[1][2][3].

IC50 & Target

Ki: 0.15 nM (glucocorticoid receptor)[1]

In Vitro

Nenocorilant (0-1000 nM; 0-72 h; OvCa cells) has pro-apoptotic effects and reverses the effects of cortisol and partially restored Paclitaxel and Gemcitabine induction of tumor-cell apoptosis[1].
Nenocorilant (100 nM; 4 h; MIA PaCa-2 and OVCAR5 cells) prevents dex-mediated upregulation of both GR target genes SGK1 and MKP1[2].

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

In Vivo

Nenocorilant (30 mg/kg; p.o.; once every four days, for 25 d; female Balb/c nude mice) improves the efficacy and promotes apoptotic activity of cytotoxic therapy in xenograft models under physiological cortisol conditions[1].

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

Animal Model: Female Balb/c nude mice[1]
Dosage: 30 mg/kg
Administration: Oral administration; once every four days, for 25 days
Result: Inhibited tumor growth and increased the expression level of caspase 3.
Clinical Trial
Molecular Weight

587.55

Formula

C26H21F4N7O3S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC(C(F)(F)F)=CC=N1)[C@@]23C(CCN(C3)S(=O)(C4=NN(N=C4)C)=O)=CC5=C(C=NN5C6=CC=C(C=C6)F)C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (170.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7020 mL 8.5099 mL 17.0198 mL
5 mM 0.3404 mL 1.7020 mL 3.4040 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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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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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 (4.25 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    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% Corn Oil

    Solubility: 2.5 mg/mL (4.25 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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
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. 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
DMSO 1 mM 1.7020 mL 8.5099 mL 17.0198 mL 42.5496 mL
5 mM 0.3404 mL 1.7020 mL 3.4040 mL 8.5099 mL
10 mM 0.1702 mL 0.8510 mL 1.7020 mL 4.2550 mL
15 mM 0.1135 mL 0.5673 mL 1.1347 mL 2.8366 mL
20 mM 0.0851 mL 0.4255 mL 0.8510 mL 2.1275 mL
25 mM 0.0681 mL 0.3404 mL 0.6808 mL 1.7020 mL
30 mM 0.0567 mL 0.2837 mL 0.5673 mL 1.4183 mL
40 mM 0.0425 mL 0.2127 mL 0.4255 mL 1.0637 mL
50 mM 0.0340 mL 0.1702 mL 0.3404 mL 0.8510 mL
60 mM 0.0284 mL 0.1418 mL 0.2837 mL 0.7092 mL
80 mM 0.0213 mL 0.1064 mL 0.2127 mL 0.5319 mL
100 mM 0.0170 mL 0.0851 mL 0.1702 mL 0.4255 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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Nenocorilant
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