Cat. No.: HY-B0340

Nefiracetam

(Synonyms: DM9384; DZL-221)

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Based on 1 Customer Validation

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.

Purity: 99.87%
CAS No.: 77191-36-7
Formula: C₁₄H₁₈N₂O₂
Molecular Weight:246.30

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Nefiracetam Chemical Structure

CAS No.: 77191-36-7

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]^[2]^[3]^[4]^[5]^[6]

N-type calcium channel

L-type calcium channel

mGlu5 Receptor

NMDA Receptor

All iGluR Isoforms :

All mGluR Isoforms :

All PKC Isoforms :

All Calcium Channel Isoforms :

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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 77191-36-7
Appearance Solid
Molecular Weight 246.30
Formula C₁₄H₁₈N₂O₂
Color White to off-white
SMILES

O=C(NC1=C(C)C=CC=C1C)CN2C(CCC2)=O
Synonyms

DM9384; DZL-221
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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.0601 mL

20.3004 mL

40.6009 mL

5 mM

0.8120 mL

4.0601 mL

8.1202 mL

10 mM

0.4060 mL

2.0300 mL

4.0601 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (10.15 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Nomura T, et al. Nefiracetam facilitates hippocampal neurotransmission by a mechanism independent of the piracetam and aniracetam action. Brain Res. 2000 Jul 7;870(1-2):157-62. [Content Brief]

[2]. Moriguchi S, et al. Nefiracetam activation of CaM kinase II and protein kinase C mediated by NMDA and metabotropic glutamate receptors in olfactory bulbectomized mice. J Neurochem. 2009 Jul;110(1):170-81. [Content Brief]

[3]. Nishizaki T, et al. A 'long-term-potentiation-like' facilitation of hippocampal synaptic transmission induced by the nootropic nefiracetam. Brain Res. 1999 May 1;826(2):281-8. [Content Brief]

[4]. Fukatsu T, et al. Effects of nefiracetam on spatial memory function and acetylcholine and GABA metabolism in microsphere-embolized rats. Eur J Pharmacol. 2002 Oct 18;453(1):59-67. [Content Brief]

[5]. Shiotani T, et al. Anticonvulsant actions of nefiracetam on epileptic EL mice and their relation to peripheral-type benzodiazepine receptors. Brain Res. 2000 Mar 24;859(2):255-61. [Content Brief]

[6]. Yoshii M, et al. Cellular mechanisms underlying cognition-enhancing actions of nefiracetam (DM-9384). Behav Brain Res. 1997 Feb;83(1-2):185-8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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All iGluR Isoforms

All mGluR Isoforms

All PKC Isoforms

All Calcium Channel Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Nefiracetam Related Classifications

HY-B0340 Related Classifications