2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. Nicergoline

Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease.

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Nicergoline Chemical Structure

Nicergoline Chemical Structure

CAS No. : 27848-84-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 37 In-stock
Solution
10 mM * 1 mL in DMSO USD 37 In-stock
Solid
5 mg USD 35 In-stock
10 mg USD 46 In-stock
25 mg USD 67 In-stock
50 mg USD 84 In-stock
100 mg USD 105 In-stock
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Based on 1 publication(s) in Google Scholar

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Nicergoline Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease[1][2].

IC50 & Target

α adrenergic receptor

 

In Vitro

Nicergoline (0.3-30 μM; 24 h) attenuates activated microglia- and astrocytes-induced neuronal cell death[3].
Nicergoline (0.3-30 μM; 48 h) suppresses the production of proinflammatory cytokines and superoxide anion by activated microglia[3].

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

Nicergoline Related Antibodies
In Vivo

Nicergoline (10 mg/kg; i.v. once daily for 60 d) improves impaired neurogenesis and cognitive competence in mice with Alzheimer's disease[2].
Nicergoline (10 mg/kg; i.v. once daily for 60 d) inhibits apoptosis, inflammation and oxidative stress in hippocampal cells, and regulates the activity of hippocampal cells through the PI3K/AKT signaling pathway in mice[2].

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

Animal Model: 3×Tg-AD mice (male, 28-35 g, 6 weeks) with the Alzheimer's disease[2]
Dosage: 10 mg/kg
Administration: I.v. once daily for 60 days
Result: Improved neurogenesis and cognitive competence.
Decreased the degree of dementia.
Downregulated pathogenic Aβ-42 and -40 peptides and APP in the hippocampi.
Increased Levels of the neuroprotective forkhead box protein P2 (Foxp2), Src homology 2-containing inositol phosphatase (SxIP) and end-binding proteins (EB) in the hippocampi.
Exhibited marked differences in the dispersion of the pyramidal cell layer between the nicergoline-treated and control groups.
Clinical Trial
Molecular Weight

484.39

Formula

C24H26BrN3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CO[C@@]([C@@]1([H])C2)(C[C@@H](COC(C3=CN=CC(Br)=C3)=O)CN1C)C4=C5C2=CN(C)C5=CC=C4
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 : 100 mg/mL (206.45 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 2.0645 mL 10.3223 mL 20.6445 mL
5 mM 0.4129 mL 2.0645 mL 4.1289 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
×
Volume
×
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 (5.16 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.16 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). 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, 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
DMSO 1 mM 2.0645 mL 10.3223 mL 20.6445 mL 51.6113 mL
5 mM 0.4129 mL 2.0645 mL 4.1289 mL 10.3223 mL
10 mM 0.2064 mL 1.0322 mL 2.0645 mL 5.1611 mL
15 mM 0.1376 mL 0.6882 mL 1.3763 mL 3.4408 mL
20 mM 0.1032 mL 0.5161 mL 1.0322 mL 2.5806 mL
25 mM 0.0826 mL 0.4129 mL 0.8258 mL 2.0645 mL
30 mM 0.0688 mL 0.3441 mL 0.6882 mL 1.7204 mL
40 mM 0.0516 mL 0.2581 mL 0.5161 mL 1.2903 mL
50 mM 0.0413 mL 0.2064 mL 0.4129 mL 1.0322 mL
60 mM 0.0344 mL 0.1720 mL 0.3441 mL 0.8602 mL
80 mM 0.0258 mL 0.1290 mL 0.2581 mL 0.6451 mL
100 mM 0.0206 mL 0.1032 mL 0.2064 mL 0.5161 mL
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Nicergoline 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:

Nicergoline27848-84-6Adrenergic ReceptorBeta Receptorbromonicotinicα1AadrenoceptorvasodilatorAlzheimer'sdiseaseInhibitorinhibitorinhibit

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