2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein Epigenetics TGF-beta/Smad
  3. nAChR iGluR mGluR PKC GABA Receptor Calcium Channel
  4. Nefiracetam

Nefiracetam  (Synonyms: DM9384; DZL-221)

Cat. No.: HY-B0340 Purity: 99.91%
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Nefiracetam is a cognition-enhancing agent. Nefiracetam is an activator of nAChR, N-methyl-D-aspartate receptor (NMDAR), mGluR5, PKC, gamma-aminobutyric acid (GABA), and N/L-type Ca2+ channels. Nefiracetam promotes neuroplasticity and enhances neuroprotection. Nefiracetam can be used in Alzheimer's disease, epilepsy, and cerebral ischemia research.

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

Nefiracetam Chemical Structure

Nefiracetam Chemical Structure

CAS No. : 77191-36-7

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Nefiracetam:

Nefiracetam Related Antibodies

Top Publications Citing Use of Products

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AMPA Receptor NMDA Receptor Kainate Receptor

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mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

  • Biological Activity

  • Purity & Documentation

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Description

Nefiracetam is a cognition-enhancing agent. Nefiracetam is an activator of nAChR, N-methyl-D-aspartate receptor (NMDAR), mGluR5, PKC, gamma-aminobutyric acid (GABA), and N/L-type Ca2+ channels. Nefiracetam promotes neuroplasticity and enhances neuroprotection. Nefiracetam can be used in Alzheimer's disease, epilepsy, and cerebral ischemia research[1][2][3][4][5][6].

IC50 & Target[1][2][3][4][5][6]

N-type calcium channel

 

L-type calcium channel

 

mGlu5 Receptor

 

NMDA Receptor

 

In Vitro

Nefiracetam (1-1000 nM, 10-60 min) increases rat dentate gyrus hippocampal neurotransmission (250%) in a dose-dependent manner[1].
Nefiracetam (1 μM, 20 min) enhances the activity of neuronal nAChR α3β2 (127%), α3β4 (124%), α4β2 (129%), α4β4 (112%), and α7 (178%) receptors in Xenopus oocytes[1].
Nefiracetam (1-1000 nM) improves NMDA receptor-dependent long-term potentiation (LTP) (64%) in the CA1 region of the hippocampus of OBX mice[2].
Nefiracetam (10 nM) enhances the autophosphorylation of CaMKIIα (Thr286) (77.3%) and PKCα (Ser657) (93.3%) in the CA1 region of the hippocampus of OBX mice[2].
Nefiracetam (1 μM) increases Ca2+ currents flowing through high voltage-activated (N/L-type) calcium channels in NG108-15 cells (more than 2 fold)[6].

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

Nefiracetam Related Antibodies
In Vivo

Nefiracetam (0.1-1.0 mg/kg, p.o.) improves spatial reference memory-related behaviors in olfactory bulbectomized (OBX) mice[2].
Nefiracetam (10 mg/kg, i.g., once a day for 3-5 days) increases the GABA content in the right hippocampus of rats with microsphere embolization[4].
Nefiracetam (10 mg/kg, i.g., once a day for 3-5 days) increases the glutamate decarboxylase activity in the right cerebral cortex and hippocampus of rats with microsphere embolization[4].
Nefiracetam (10 mg/kg, p.o., once) inhibits Ro 5-4864 (PBR activator)-induced convulsions in EL (Epilepsy-prone Lesion) mice in a dose-dependent manner (ED50: 17.2 mg/kg) [5].
Nefiracetam (10 mg/kg, p.o., once) inhibits Ro 5-4864-induced convulsions in DDY mice (parental strain of EL mice) and spontaneous epilepsy in EL mice in a dose-dependent manner[5].

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

Animal Model: OBX mice (male, 8-9 weeks old)[2]
Dosage: 0.1, 0.5, 1.0 mg/kg; 1, 10, 100, 1000 nM
Administration: Oral gavage (p.o.)
Result: Recovered the percentage of alteration behavior (64%).
Had no change in the total number of arms entries.
Induced enhanced levels of LTP in HFS in a dose-dependent manner.
Animal Model: Microsphere embolization rat model (male Wistar rats, 180-220 g)[4]
Dosage: 10 mg/kg
Administration: Intragastric administration (i.g.), once every day for 3 and 5 d
Result: Increased GABA content in the right hippocampus.
Increased glutamate decarboxylase activity in the right cerebral cortex and hippocampus.
Animal Model: EL mice model (adult male mice, 25-30 g)[5]
Dosage: 10 mg/kg
Administration: Oral gavage (p.o.); Intravenous injection (i.v.), once
Result: Inhibited Ro 5-4864-induced convulsions.
Inhibited spontaneous epilepsy in EL mice.
Animal Model: DDY mice model (adult male mice, 30-35 g)[5]
Dosage: 10 mg/kg
Administration: Intravenous injection (i.v.), once
Result: Inhibited Ro 5-4864-induced convulsions in DDY mice.
Clinical Trial
Molecular Weight

246.30

Formula

C14H18N2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=C(C)C=CC=C1C)CN2C(CCC2)=O
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 (406.01 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 25 mg/mL (101.50 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0601 mL 20.3004 mL 40.6009 mL
5 mM 0.8120 mL 4.0601 mL 8.1202 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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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

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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 (10.15 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 (10.15 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.
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, 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
H2O / DMSO 1 mM 4.0601 mL 20.3004 mL 40.6009 mL 101.5022 mL
5 mM 0.8120 mL 4.0601 mL 8.1202 mL 20.3004 mL
10 mM 0.4060 mL 2.0300 mL 4.0601 mL 10.1502 mL
15 mM 0.2707 mL 1.3534 mL 2.7067 mL 6.7668 mL
20 mM 0.2030 mL 1.0150 mL 2.0300 mL 5.0751 mL
25 mM 0.1624 mL 0.8120 mL 1.6240 mL 4.0601 mL
30 mM 0.1353 mL 0.6767 mL 1.3534 mL 3.3834 mL
40 mM 0.1015 mL 0.5075 mL 1.0150 mL 2.5376 mL
50 mM 0.0812 mL 0.4060 mL 0.8120 mL 2.0300 mL
60 mM 0.0677 mL 0.3383 mL 0.6767 mL 1.6917 mL
80 mM 0.0508 mL 0.2538 mL 0.5075 mL 1.2688 mL
100 mM 0.0406 mL 0.2030 mL 0.4060 mL 1.0150 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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Nefiracetam Related Classifications

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  • 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:

Nefiracetam77191-36-7DM9384 DZL-221DM 9384DM-9384DZL221DZL 221DZL-221nAChRiGluRmGluRPKCGABA ReceptorCalcium ChannelNicotinic acetylcholine receptorsIonotropic glutamate receptorsMetabotropic glutamate receptorsProtein kinase CGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorCa2+ channelsCa channelscognition-enhancingOBX micemicrosphere embolization rat modelEL miceRo 5-4864Alzheimer's diseaseepilepsycerebral ischemiaInhibitorinhibitorinhibit

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