Fasoracetam
Based on 1 Customer Validation
Fasoracetam (NS105) is an orally active metabotropic glutamate receptor (mGluR) activator. Fasoracetam bidirectionally regulates adenylyl cyclase activity and cAMP levels by activating group I-III mGluRs, upregulating GABAB receptors, and enhancing cholinergic neurotransmission. Fasoracetam can be used in research on attention deficit hyperactivity disorder (ADHD), depression, dementia, Alzheimer's disease, and forebrain ischemia.
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- Purity : 99.41%
- CAS No.: 110958-19-5
- 화학식: C10H16N2O2
- 분자량:196.25
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[2]|
mGluR 1 |
mGluR2 |
mGluR3 |
In Vitro
Fasoracetam (NS-105) (0.1-1 μM; 15 min) bidirectionally modulates adenylyl cyclase in rat brain cortical membranes, inhibiting Forskolin (HY-15371)-stimulated cAMP via group II/III mGlu receptors at 0.1 μM and promoting cAMP via group I mGlu receptors at 1 μM in Forskolin-pretreated membranes[2].
Fasoracetam (0.1-1 μM; 15 min) exhibits activity in promoting forskolin-stimulated cAMP production in PTX-pretreated rat cerebral cortex cell membranes[2].
Fasoracetam (1 μM; 10-60 min) increases [35S]GTPγS binding in intact cell membranes of rat cerebral cortex[3].
Fasoracetam (10 nM-1 μM; 10 min) has activity in enhancing Isoproterenol (HY-B0468)-stimulated cAMP accumulation in rat cerebral cortex slices[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Fasoracetam (1-100 mg/kg; p.o.; single administration; 40 min before testing) ameliorates memory impairment in a Baclofen (HY-B0007)-induced passive avoidance memory disruption model in Wistar rats[4].
Fasoracetam (3-30 mg/kg; p.o.; single administration; immediately after electroconvulsive shock) prevents memory impairment in a Wistar rat model of electroconvulsive shock (ECS)-induced memory disruption[4].
Fasoracetam (10-100 mg/kg; p.o.; once daily; 14 days) reverses memory impairment in AF64A- or cerebral ischemia-induced radial arm maze Wistar rat models[4].
Fasoracetam (10 mg/kg; p.o.; single administration) increases cerebral cortical acetylcholine (ACh) release in awake, freely moving Wistar rats[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male, 5 weeks old) (Scopolamine-, electrolytic NBM lesion-, AF64A-, Baclofen-, cerebral ischemia-, and electroconvulsive shock (ECS)-induced memory disruption)[4]
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Dosage:1, 10, 30, 100, 300 mg/kg
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Administration:p.o.; single dose or once daily for 14 days
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Result:Significantly reversed or prevented passive avoidance memory deficits induced by various cholinergic dysfunctions, baclofen, or ECS, and significantly ameliorated learning and memory impairments in the radial arm maze test in AF64A- or cerebral ischemia-treated rats.
Chemical Information
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CAS No. 110958-19-5
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Appearance Solid
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분자량 196.25
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화학식 C10H16N2O2
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Color White to off-white
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SMILES
O=C([C@@H]1NC(CC1)=O)N2CCCCC2
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Synonyms
NS 105
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 250 mg/mL (1273.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (10.60 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (10.60 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
순도&문서
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Data Sheet (286 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Elia J, et al. Fasoracetam in adolescents with ADHD and glutamatergic gene network variants disrupting mGluR neurotransmitter signaling. Nature communications. 2018 Jan 16;9(1):4. [Content Brief]
[5]. Shorvon S. Pyrrolidone derivatives. The Lancet. 2001 Dec 1;358(9296):1885-92. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 5.0955 mL | 25.4777 mL | 50.9554 mL | 127.3885 mL |
| 5 mM | 1.0191 mL | 5.0955 mL | 10.1911 mL | 25.4777 mL | |
| 10 mM | 0.5096 mL | 2.5478 mL | 5.0955 mL | 12.7389 mL | |
| 15 mM | 0.3397 mL | 1.6985 mL | 3.3970 mL | 8.4926 mL | |
| 20 mM | 0.2548 mL | 1.2739 mL | 2.5478 mL | 6.3694 mL | |
| 25 mM | 0.2038 mL | 1.0191 mL | 2.0382 mL | 5.0955 mL | |
| 30 mM | 0.1699 mL | 0.8493 mL | 1.6985 mL | 4.2463 mL | |
| 40 mM | 0.1274 mL | 0.6369 mL | 1.2739 mL | 3.1847 mL | |
| 50 mM | 0.1019 mL | 0.5096 mL | 1.0191 mL | 2.5478 mL | |
| 60 mM | 0.0849 mL | 0.4246 mL | 0.8493 mL | 2.1231 mL | |
| 80 mM | 0.0637 mL | 0.3185 mL | 0.6369 mL | 1.5924 mL | |
| 100 mM | 0.0510 mL | 0.2548 mL | 0.5096 mL | 1.2739 mL |
Fasoracetam Related Classifications
HY-107481 Related Classifications
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