(S)-(-)-5-Fluorowillardiine hydrochloride
Based on 1 Customer Validation
(S)-(-)-5-Fluorowillardiine ((5S)-Fluorowillardiine; (S)-5-Fluorowillardiine) hydrochloride is a potent, highly selective non-NMDA ionotropic glutamate receptor (iGluR, AMPA/Kainate receptor) agonist. (S)-(-)-5-Fluorowillardiine hydrochloride activates high-affinity AMPA-preferring receptors (EC50 = 0.70 μM) and low-affinity kainate-preferring receptors (EC50 = 170 μM), thereby inducing biphasic dose-dependent neurotoxicity/excitotoxicity. (S)-(-)-5-Fluorowillardiine hydrochloride is applicable to research related to schizophrenia, temporal lobe epilepsy, and bipolar disorder.
For research use only. We do not sell to patients.
- Purity : 99.03%
- CAS No.: 1321546-70-6
- Formula: C7H9ClFN3O4
- Molecular Weight:253.62
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
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AMPA Receptor |
In Vitro
(S)-(-)-5-Fluorowillardiine (10-100 μM; 24 h) hydrochloride induces > 90% neurotoxicity in primary cultured murine cortical neurones via a biphasic mechanism, with high-affinity component activity at AMPA receptors (EC50 = 0.70 μM) and low-affinity component activity at kainate receptors (EC50 = 170 μM)[1].
(S)-(-)-5-Fluorowillardiine (200 nM-60 μM) hydrochloride potently activates AMPA/kainate receptors on primary dissociated cultures of mouse embryonic hippocampal neurons with an equilibrium EC50 of 1.47 μM, induces strong desensitization (92.5%), exhibits cross-desensitization with other willardiine derivatives, and produces a prolonged inward tail current following agonist removal[2].
(S)-(-)-5-Fluorowillardiine (0.1 nM-1 mM; 2 h) hydrochloride binds to mouse GluK5 kainate receptor subunits expressed in Sf9 cell membranes with a Ki of 1.79 μM, and exhibits similar affinity for GluK5 and GluK1 subunits[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1321546-70-6
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Appearance Solid
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Molecular Weight 253.62
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Formula C7H9ClFN3O4
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Color White to off-white
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SMILES
OC([C@@H](N)CN1C=C(F)C(NC1=O)=O)=O.[H]Cl
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Synonyms
(5S)-Fluorowillardiine hydrochloride; (S)-5-Fluorowillardiine hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
H2O : 6.67 mg/mL (26.30 mM; Need ultrasonic)
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)
Purity & Documentation
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Data Sheet (275 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]. Larm JA, et al. (S)-5-fluorowillardiine-mediated neurotoxicity in cultured murine cortical neurones occurs via AMPA and kainate receptors. Eur J Pharmacol. 1996;314(1-2):249-254. [Content Brief]
[2]. Patneau DK, et al. Activation and desensitization of AMPA/kainate receptors by novel derivatives of willardiine. J Neurosci. 1992;12(2):595-606. [Content Brief]
[3]. Møllerud S, et al. A pharmacological profile of the high-affinity GluK5 kainate receptor. Eur J Pharmacol. 2016;788:315-320. [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 |
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| H2O | 1 mM | 3.9429 mL | 19.7145 mL | 39.4291 mL | 98.5727 mL |
| 5 mM | 0.7886 mL | 3.9429 mL | 7.8858 mL | 19.7145 mL | |
| 10 mM | 0.3943 mL | 1.9715 mL | 3.9429 mL | 9.8573 mL | |
| 15 mM | 0.2629 mL | 1.3143 mL | 2.6286 mL | 6.5715 mL | |
| 20 mM | 0.1971 mL | 0.9857 mL | 1.9715 mL | 4.9286 mL | |
| 25 mM | 0.1577 mL | 0.7886 mL | 1.5772 mL | 3.9429 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.
(S)-(-)-5-Fluorowillardiine hydrochloride Related Classifications
HY-16713A Related Classifications
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