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Dimiracetam

Alias: ISF-4185 BND-11624 BND11624 ISF4185 NT 11624NT-11624NT-11624 BND-11624 ISF-4185 NT11624 BND 11624 ISF 4185
Cat No.:V19981 Purity: ≥98%
Dimiracetam (NT-11624; BND11624; ISF-4185) is a novel and potent NMDA-receptor antagonist with potential to be used for the treatment of neuropathic pain.
Dimiracetam
Dimiracetam Chemical Structure CAS No.: 126100-97-8
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
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Product Description
Dimiracetam (NT-11624; BND11624; ISF-4185) is a novel and potent NMDA-receptor antagonist with potential to be used for the treatment of neuropathic pain.
Dimiracetam (CAS# 126100-97-8) is an orally active compound belonging to the racetam family of nootropic drugs with anti-neuropathic activity. It inhibits hypersensitivity and neurological alterations and inhibits Sorafenib-induced neuropathy in cold stimulation rat models. The compound functions by modulating neurotransmission, particularly through interactions with glutamatergic and cholinergic systems, which play crucial roles in learning and memory processes. Dimiracetam has shown promise in the treatment of neuropathic pain, cognitive disorders, and depression.
Biological Activity I Assay Protocols (From Reference)
Targets
N-methyl-D-aspartate receptor (NMDAR) antagonist. Dimiracetam modulates neurotransmission through interactions with glutamatergic and cholinergic systems.
ln Vitro
Dimiracetam inhibits hypersensitivity and neurological alterations in vitro. It modulates neurotransmission through interactions with glutamatergic and cholinergic systems, which are crucial for learning and memory processes. The compound has shown promise in the treatment of neuropathic pain and cognitive disorders.
ln Vivo
Dimiracetam is orally active with anti-neuropathic activity. It inhibits Sorafenib-induced neuropathy in cold stimulation rat models. The compound inhibits hypersensitivity and neurological alterations. It has shown promise in treating neuropathic pain, cognitive disorders, and depression.
Enzyme Assay
Dimiracetam's activity is typically assessed in receptor binding assays targeting the N-methyl-D-aspartate receptor (NMDAR). Standard radioligand binding techniques using membrane preparations from brain tissue or cells expressing recombinant NMDARs and radiolabeled NMDAR ligands are used to determine binding affinity and antagonist activity.
Cell Assay
In vitro cell-based assays for dimiracetam evaluate its neuroprotective and anti-neuropathic effects in neuronal cell cultures. Primary neurons or neuronal cell lines are subjected to neurotoxic or neuropathic stimuli (such as chemotherapeutic agents) in the presence or absence of the compound. Neuronal survival, neurite outgrowth, and markers of neuronal damage are assessed.
Animal Protocol
In vivo animal studies for dimiracetam have been conducted in rat models of chemotherapy-induced neuropathy. Sorafenib is administered to induce neuropathy, and the compound is given orally to evaluate its protective effects. Cold stimulation tests are used to assess hypersensitivity as the primary endpoint. Other models of neuropathic pain and cognitive impairment are also used.
ADME/Pharmacokinetics
Dimiracetam is orally active. It has a molecular weight of approximately 226.23 g/mol. Detailed pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution are not extensively reported in the provided literature. The compound is soluble in DMSO and other organic solvents.
Toxicity/Toxicokinetics
Specific toxicity data for dimiracetam is not extensively reported. As a compound belonging to the racetam family, it is expected to have a relatively favorable safety profile based on the known safety of other racetam compounds. The compound is classified as a research-grade chemical and is not intended for human use.
References

[1]. A model of neuropathic pain induced by sorafenib in the rat: Effect of dimiracetam. Neurotoxicology. 2015 Sep;50:101-7.

[2]. A rat model of FOLFOX-induced neuropathy: effects of oral dimiracetam in comparison with duloxetine and pregabalin. Cancer Chemother Pharmacol. 2017 Dec;80(6):1091-1103.

Additional Infomation
Dimiracetam has been used in trials to study the treatment of AIDS, neuropathy, and acquired immunodeficiency syndrome.
Dimiracetam (CAS# 126100-97-8) is an orally active nootropic compound belonging to the racetam family with anti-neuropathic activity. It targets the NMDAR as an antagonist and modulates glutamatergic and cholinergic neurotransmission. The compound inhibits hypersensitivity and neurological alterations, and inhibits Sorafenib-induced neuropathy in cold stimulation rat models. It has shown promise in treating neuropathic pain, cognitive disorders, and depression. It has not received FDA approval.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C6H8N2O2
Molecular Weight
140.14
Exact Mass
140.059
CAS #
126100-97-8
PubChem CID
65955
Appearance
Light yellow to yellow solid powder
Density
1.4g/cm3
Boiling Point
460.5ºC at 760 mmHg
Flash Point
232.3ºC
Vapour Pressure
1.16E-08mmHg at 25°C
Index of Refraction
1.585
LogP
-0.9
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
2
Rotatable Bond Count
0
Heavy Atom Count
10
Complexity
202
Defined Atom Stereocenter Count
0
InChi Key
XTXXOHPHLNROBN-UHFFFAOYSA-N
InChi Code
InChI=1S/C6H8N2O2/c9-5-3-8-4(7-5)1-2-6(8)10/h4H,1-3H2,(H,7,9)
Chemical Name
tetrahydro-5H-pyrrolo[1,2-a]imidazole-2,5(3H)-dione
Synonyms
ISF-4185 BND-11624 BND11624 ISF4185 NT 11624NT-11624NT-11624 BND-11624 ISF-4185 NT11624 BND 11624 ISF 4185
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 : ~125 mg/mL (~891.97 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (14.84 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 20.8 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: ≥ 2.08 mg/mL (14.84 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 20.8 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: ≥ 2.08 mg/mL (14.84 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 20.8 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 7.1357 mL 35.6786 mL 71.3572 mL
5 mM 1.4271 mL 7.1357 mL 14.2714 mL
10 mM 0.7136 mL 3.5679 mL 7.1357 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.

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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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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
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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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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