NNC-711
Based on 1 Customer Validation
NNC-711 (NO-711 hydrochloride) is a potent and selective inhibitor of GAT-1 (GABA transporter 1) with IC50 values of 0.04, 0.38, 171, 1700, 349, 622 μM for human GAT-1, rat GAT-1, rGAT-2, hGAT-3, rGAT-3, hBGT-3, respectively. NNC-711 has anticonvulsant and analgesic effect in vivo and exhibits cognition-enhancing activity.
For research use only. We do not sell to patients.
- Purity: 99.76%
- CAS No.: 145645-62-1
- Formula: C21H23ClN2O3
- Molecular Weight:386.87
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Bioactive Compound Library Max
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Bioactive Compound Library
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Membrane Transporter/Ion Channel Compound Library
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Neuronal Signaling Compound Library
HY-L013
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Neurotransmitter Receptor Compound Library
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Anti-Alzheimer's Disease Compound Library
HY-L069
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Anti-Parkinson's Disease Compound Library
HY-L085
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Neurodegenerative Disease-related Compound Library
HY-L086
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GABA Receptor Compound Library
HY-L120
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
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Highly Selective Inhibitors Library
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Ion Channel Compound Library
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MCE Bioactive Compound Library
HY-L001V
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
NNC-711 is a potent inhibitor of [3H]GABA uptake in vitro in both rat brain synaptosomes (IC50 = 47 nM), and neuronal (IC50 = 1238 nM) and glial (IC50 = 636 nM) elements[4].
NNC-711 displaces [3H]tiagabine binding from the GABA uptake carrier in vitro (IC50 = 20 nM)[4].
NNC-711 (1 μM, 0-15 min) significantly reduces Na+-dependent GABA uptake in microglial cell[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
NNC-711 (0.5-3 mg/kg; i.p.; immediately prior to occlusion) protects against ischemia-induced death of CA1 pyramidal neurons in a model of bilateral common carotid artery occlusion in the gerbil[2].
NNC-711 (0.5-1.5 mg/kg; i.p.; immediately prior to training) exhibits significant cognition-enhancing actions in postnatal day 80 male and 28-month old female Wistar rats[2].
NNC-711 (NO-711) (50-200 μg/10 μL; i.t.; once) effectively develops analgesic effect in sciatic nerve CCI rats modelc[3].
NNC-711 (0.3-30 mg/kg, i.p.; 30 min before testing) exhibits anticonvulsant effects in Multiple mices and rats epilepsy model[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DMCM (HY-100369A)-induced seizures in female NMRI mice (20 g), pentylenetetrazole-induced seizures in male NMRI mice and male albino Wistar SPF rats (150-200 g), Audiogenic seizures in male DBA/2 mice (8 g) [4]
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Dosage:0.3-30 mg/kg
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Administration:Intraperitoneal injection (i.p.); 30 min prior to the seizure test
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Result:Inhibited DMCM-induced clonic seizures in NMRI mice with an ED50 = 1.2 mg/kg.
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Animal Model:Postnatal day 80 male Wistar rats (300-350 g)[2]
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Dosage:0.25, 0.5, 1, 3 mg/kg
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Administration:Intraperitoneal injection (i.p.); 30 min prior to training
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Result:Significantly reversed the amnesia induced by scopolamine administration 6-h post-training when retrieval was tested at 24-h post-training.
Had no effect on learning in the 0.25-0.5 mg/kg dose range, and induced amnesia at 3.0 mg/kg.
Not to directly interact with the cholinergic system, but rather to have a more general neuroprotective action on the consolidation process.
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Animal Model:Postnatal day 80 male Mongolian gerbils (50-65 g)[2]
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Dosage:0.5, 3 mg/kg
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Administration:Intraperitoneal injection (i.p.); immediately prior to occlusion
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Result:Administrated immediately prior to occlusion significantly reduced CA1 cell death.
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Animal Model:Postnatal day 80 male Wistar rats (300-350 g) and 28-month old female Wistar rats[2]
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Dosage:0.5, 1.5 mg/kg
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Administration:Intraperitoneal injection (i.p.); immediately prior to training
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Result:Significantly reduced escape latencies in both mature postnatal day 80 and aged 28 months rats.
Improved rats ability to locate the hidden platform at 0.5 mg/kg, but the effect was reduced at 1.5 mg/kg.
Had no effect on memory retention.
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Animal Model:Sciatic nerve chronic constriction injury (CCI) rats[3]
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Dosage:50, 100, 200 μg/10 μL
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Administration:Intrathecal (i.t.); once
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Result:Increased withdrawal thresholds (WT) and withdrawal latency (WL) values after 1 day compared with CCI + saline group.
The maximum value of WT was achieved 3 days after administration and maximum value of WL was achieved 1 day after administration.
Chemical Information
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CAS No. 145645-62-1
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Appearance Solid
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Molecular Weight 386.87
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Formula C21H23ClN2O3
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Color White to off-white
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SMILES
O=C(C1=CCCN(CCO/N=C(C2=CC=CC=C2)\C3=CC=CC=C3)C1)O.[H]Cl
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Synonyms
NO-711 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (258.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 4 mg/mL (10.34 mM; Need ultrasonic and warming)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* 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.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.46 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Borden LA, et al. Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. Eur J Pharmacol. 1994 Oct 14;269(2):219-24. [Content Brief]
[2]. O'Connell AW, et al. Anti-ischemic and cognition-enhancing properties of NNC-711, a gamma-aminobutyric acid reuptake inhibitor. Eur J Pharmacol. 2001 Jul 13;424(1):37-44. [Content Brief]
[3]. Li Y,et al. Analgesic effect of intrathecally γ-aminobutyric acid transporter-1 inhibitor NO-711 administrating on neuropathic pain in rats. Neurosci Lett. 2011 Apr 20;494(1):6-9. [Content Brief]
[4]. Suzdak PD, et al. NNC-711, a novel potent and selective gamma-aminobutyric acid uptake inhibitor: pharmacological characterization. Eur J Pharmacol. 1992 Dec 2;224(2-3):189-98. [Content Brief]
[5]. Fattorini G, et al. Microglial expression of GAT-1 in the cerebral cortex. Glia. 2020 Mar;68(3):646-655. [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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.5848 mL | 12.9242 mL | 25.8485 mL | 64.6212 mL |
| 5 mM | 0.5170 mL | 2.5848 mL | 5.1697 mL | 12.9242 mL | |
| 10 mM | 0.2585 mL | 1.2924 mL | 2.5848 mL | 6.4621 mL | |
| DMSO | 15 mM | 0.1723 mL | 0.8616 mL | 1.7232 mL | 4.3081 mL |
| 20 mM | 0.1292 mL | 0.6462 mL | 1.2924 mL | 3.2311 mL | |
| 25 mM | 0.1034 mL | 0.5170 mL | 1.0339 mL | 2.5848 mL | |
| 30 mM | 0.0862 mL | 0.4308 mL | 0.8616 mL | 2.1540 mL | |
| 40 mM | 0.0646 mL | 0.3231 mL | 0.6462 mL | 1.6155 mL | |
| 50 mM | 0.0517 mL | 0.2585 mL | 0.5170 mL | 1.2924 mL | |
| 60 mM | 0.0431 mL | 0.2154 mL | 0.4308 mL | 1.0770 mL | |
| 80 mM | 0.0323 mL | 0.1616 mL | 0.3231 mL | 0.8078 mL | |
| 100 mM | 0.0258 mL | 0.1292 mL | 0.2585 mL | 0.6462 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.
NNC-711 Related Classifications
HY-103506 Related Classifications
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