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Aniracetam

Cat No.:V11330 Purity: ≥98%
Aniracetam (Ro 13-5057) is an orally bioactive neuro-protective (neuro-protection) agent with nootropic activity.
Aniracetam
Aniracetam Chemical Structure CAS No.: 72432-10-1
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
500mg
1g
5g
Other Sizes
Official Supplier of:
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Product Description
Aniracetam (Ro 13-5057) is an orally bioactive neuro-protective (neuro-protection) agent with nootropic activity. Aniracetam enhances the ion shift quisqualate (iQA) response in the CA1 region of rat hippocampal slices. Aniracetam also potentiates excitatory postsynaptic potentials (EPSPs) at Schaffer's parasynaptic association synapses. Aniracetam can prevent CO2-induced learning impairment in hypercapnic model rats. Aniracetam may be utilized to study brain dysfunction.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
Aniracetam significantly enhances various concentrations of cisternic acid and counteracts cell death caused by glutamate, kainic acid, or α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid. In primary cultures of cerebellar granule cells, ester and trans-1-aminocyclopentane-1,3-dicarboxylate also produce a neuroprotective response [4]. In cerebellar granule cell primary cultures, aniracetam improves phospholipase C's mGluR-coupled stimulation [4].
ln Vivo
Aniracetam (1 mM; 30-75 min) potentiates iQA receptors and greatly increases native synaptic transmission in rats [1]. Aniracetam (10-100 mg/kg; oral; single dosage) protects CO2-induced learning impairment in rats [2]. Aniracetam (30-300 mg/kg; oral; single dosage) increases the percentage of rats demonstrating passive avoidance [2].
Animal Protocol
Animal/Disease Models: Pyramidal neurons from male Wistar rats [1]
Doses: 1 mM
Route of Administration: 30-75 minutes
Experimental Results: Enhanced iQA receptors present in the brain and produced significant facilitation of native synaptic transmission .

Animal/Disease Models: Male rat (100-120 g; pure CO2 induces hypercapnia) [2]
Doses: 10, 30, 50 and 100 mg/kg
Route of Administration: Oral; single dose (60 days before hypercapnia) minutes)
Experimental Results: CO2-induced acquisition impairment was Dramatically prevented at doses of 30 and 50 mg/kg.

Animal/Disease Models: Male rats and male mice (100-120 g and 21-25 g; 0.5 mg/kg scopolamine-induced transient memory impairment of passive avoidance procedures) [2] Doses: 30, 50, 100 and 300 mg/kg ,
Route of Administration: po; single dose
Experimental Results: 2 hrs (hrs (hours)) after 50 and 100 mg/kg scopolamine, the percentage of rats showing passive avoidance increased Dramatically.
ADME/Pharmacokinetics
Biological Half-Life
1-2.5 hours
References

[1]. Allosteric potentiation of quisqualate receptors by a nootropic drug aniracetam. J Physiol. 1990 May;424:533-43.

[2]. Effects of the novel compound aniracetam (Ro 13-5057) upon impaired learning and memory in rodents. Psychopharmacology (Berl). 1982;78(2):104-11.

[3]. Nakamura K. Aniracetam: its novel therapeutic potential in cerebral dysfunctional disorders based on recent pharmacological discoveries. CNS Drug Rev. 2002 Spring;8(1):70-89.

[4]. Attenuation of excitatory amino acid toxicity by metabotropic glutamate receptor agonists and aniracetam in primary cultures of cerebellar granule cells. J Neurochem. 1993 Aug;61(2):683-9.

[5]. Anxiolytic effects of aniracetam in three different mouse models of anxiety and the underlying mechanism. Eur J Pharmacol. 2001 May 18;420(1):33-43.

[6]. Aniracetam reversed learning and memory deficits following prenatal ethanol exposure by modulating functions of synaptic AMPA receptors. Neuropsychopharmacology. 2008 Apr;33(5):1071-83. Epub 2007 Jul 4.

Additional Infomation
Aniracetam is a member of pyrrolidin-2-ones and a N-acylpyrrolidine.
Compound with anti-depressive properties used as a mental performance enhancer.
Pharmacodynamics
Aniracetam possesses a wide range of anxiolytic properties, which may be mediated by an interaction between cholinergic, dopaminergic and serotonergic systems.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C12H13NO3
Molecular Weight
219.2365
Exact Mass
219.089
CAS #
72432-10-1
PubChem CID
2196
Appearance
White to off-white solid powder
Density
1.2±0.1 g/cm3
Boiling Point
399.7±34.0 °C at 760 mmHg
Melting Point
−58 °C(lit.)
Flash Point
195.5±25.7 °C
Vapour Pressure
0.0±0.9 mmHg at 25°C
Index of Refraction
1.574
LogP
0.27
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
3
Rotatable Bond Count
2
Heavy Atom Count
16
Complexity
282
Defined Atom Stereocenter Count
0
InChi Key
ZXNRTKGTQJPIJK-UHFFFAOYSA-N
InChi Code
InChI=1S/C12H13NO3/c1-16-10-6-4-9(5-7-10)12(15)13-8-2-3-11(13)14/h4-7H,2-3,8H2,1H3
Chemical Name
1-(4-methoxybenzoyl)pyrrolidin-2-one
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ≥ 100 mg/mL (~456.12 mM)
H2O : ~0.33 mg/mL (~1.51 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (11.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (11.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 4.5612 mL 22.8061 mL 45.6121 mL
5 mM 0.9122 mL 4.5612 mL 9.1224 mL
10 mM 0.4561 mL 2.2806 mL 4.5612 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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