AA43279
Based on 1 Customer Validation
AA43279 is an orally effective, blood-brain barrier-penetrant Nav1.1 voltage-gated sodium channel activator with an EC50 of 9.5 μM in HEK-293 cells. AA43279 inhibits fast inactivation and enhances sodium conductance. AA43279 can be used in research on schizophrenia and Dravet syndrome.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.00%
- CAS. Nr.: 354812-16-1
- Formel: C12H12N2O2S
- Molecular Weight:248.31
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Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[3]|
Nav1.1 9.5 μM (EC50) |
Nav1.6 11.6 μM (EC50) |
Nav1.5 14.4 μM (EC50) |
Nav1.2 22.8 μM (EC50) |
In Vitro
AA43279 inhibits A2A, A3, 5HT2B, NET, and MAO A in binding/enzymatic assays, with IC50 values of 21-30 μM for A2A; 11 μM for A3; 4.3 μM for 5HT2B; 3.2 μM for NET; and 2.6 μM for MAO A[3].
AA43279 (6 min) activates human Nav1.1 in HEK-293 cells with an EC50 of 9.5 μM and 2.6× potency, whereas it shows weaker activity against Nav1.2 (EC50 22.8 μM), Nav1.5 (EC50 14.4 μM), and Nav1.6 (EC50 11.6 μM), and has no enhancing effect on Nav1.4 or Nav1.7 at concentrations up to 30 μM[3].
AA43279 (30 μM; 40 min) increases the excitability of rat hippocampal CA1 parvalbumin-positive fast-spiking interneurons by hyperpolarizing the AP threshold and increasing spike output[3].
AA43279 (30 μM; 30 min) increases sIPSC frequency and amplitude in rat CA1 pyramidal neurons when glutamatergic input is intact[3].
AA43279 reduces the amplitude of Schaffer collateral-evoked synaptic potentials in CA1 pyramidal neurons and blocks further CBD modulation, indicating a convergent NaV1.1-mediated mechanism[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AA43279 (30-300 mg/kg; oral; single administration; 30 minutes after administration) exhibits in vivo anticonvulsant activity in the mouse MEST test[3].
AA43279 (10-250 µM; bath immersion/immersion; single; 20 min) increases locomotor activity at 100 µM and induces type 2 seizure-like electrographic activity at 10 and 100 µM in healthy wild-type zebrafish larvae[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NMRI (20-24 g)[3]
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Dosage:30 mg/kg, 100 mg/kg, and 300 mg/kg
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Administration:p.o. (oral gavage); single administration; 30 min post-dose
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Result:Produced an anti-convulsive effect by increasing the current impact needed to provoke convulsion.
Significant anticonvulsive effects were obtained at 300 mg/kg.
The anticonvulsive effect of 300 mg/kg AA43279 was confirmed in a separate experiment on another test day.
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Animal Model:wild-type TL (5 dpf larvae)[4]
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Dosage:10 µM, 100 µM, or 250 µM
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Administration:bath/immersion in embryo medium; single 20 min incubation
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Result:Increased swim velocities in WT larvae at 100 µM.
Representative tracking plots showed increased average swim velocity after AA43279.
In LFP recordings, AA43279 at 10 and 100 µM evoked type 2 ictal-like events in WT controls.
AA43279 showed increased electrical activity compared with DMSO-treated controls.
Chemical Information
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CAS. Nr. 354812-16-1
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Appearance Solid
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Molecular Weight 248.31
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Formel C12H12N2O2S
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Color Light yellow to light brown
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SMILES
O=C(C1=C(N)C=C(C2=CC=C(OC)C=C2)S1)N
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 6.67 mg/mL (26.86 mM; ultrasonic and warming and heat to 60°C; 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 (protect from light). 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (289 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)
Verweise
[1]. Botella H. Molecular Mapping of the Binding Sites of a Nav1. 1 Activator.
[2]. Weuring WJ, et al. NaV1.1 and NaV1.6 selective compounds reduce the behavior phenotype and epileptiform activity in a novel zebrafish model for Dravet Syndrome. PloS one. 2020;15(3):e0219106. [Content Brief]
[3]. Frederiksen K, et al. A small molecule activator of Nav1. 1 channels increases fast‐spiking interneuron excitability and GABAergic transmission in vitro and has anti‐convulsive effects in vivo. European Journal of Neuroscience. 2017 Aug;46(3):1887-96. [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 (protect from light). 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 |
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| DMSO | 1 mM | 4.0272 mL | 20.1361 mL | 40.2722 mL | 100.6806 mL |
| 5 mM | 0.8054 mL | 4.0272 mL | 8.0544 mL | 20.1361 mL | |
| 10 mM | 0.4027 mL | 2.0136 mL | 4.0272 mL | 10.0681 mL | |
| 15 mM | 0.2685 mL | 1.3424 mL | 2.6848 mL | 6.7120 mL | |
| 20 mM | 0.2014 mL | 1.0068 mL | 2.0136 mL | 5.0340 mL | |
| 25 mM | 0.1611 mL | 0.8054 mL | 1.6109 mL | 4.0272 mL |
AA43279 Related Classifications
HY-125928 Related Classifications
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Keywords
- AA43279
- 354812-16-1
- AA 43279
- AA-43279
- Sodium Channel
- CA1 pyramidal neurons
- Dravet syndrome
- Nav1.1 voltage-gated sodium channel
- epileptiform activity
- fast inactivation
- inhibitory postsynaptic currents
- parvalbumin-positive fast-spiking GABAergic interneurons
- schizophrenia
- sodium conductance
- zebrafish
- Inhibitor
- inhibitor
- inhibit