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Cat. No.: HY-16713

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(S)-(-)-5-Fluorowillardiine

Name: (S)-(-)-5-Fluorowillardiine
Brand: MedChemExpress
SKU: HY-16713
Price: 112.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: (5S)-Fluorowillardiine; (S)-5-Fluorowillardiine)

(S)-(-)-5-Fluorowillardiine ((5S)-Fluorowillardiine; (S)-5-Fluorowillardiine) is a potent, highly selective non-NMDA ionotropic glutamate receptor (iGluR, AMPA/Kainate receptor) agonist. (S)-(-)-5-Fluorowillardiine 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 is applicable to research related to schizophrenia, temporal lobe epilepsy, and bipolar disorder.

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CAS No.: 140187-23-1
Formule: C₇H₈FN₃O₄
Masse moléculaire:217.15

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

(S)-(-)-5-Fluorowillardiine Chemical Structure

CAS No.: 140187-23-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

AMPA Receptor

Voir tous les produits spécifiques à Isoform iGluR :

Cellular Effect

Cell Line	Type	Value	Description	References
Oocyte	EC₅₀	0.38 μM Compound: (S)-2b	Agonist activity at cyclothiazide-desensitized rat recombinant flip iGluR1 expressed in Xenopus laevis oocytes by two electrode voltage-clamp electrophysiology method Agonist activity at cyclothiazide-desensitized rat recombinant flip iGluR1 expressed in Xenopus laevis oocytes by two electrode voltage-clamp electrophysiology method	[PMID: 18811139]
Oocyte	EC₅₀	0.38 μM Compound: (S)-F-Willardiine	Agonist activity at recombinant GluA1 receptor expressed in Xenopus oocytes Agonist activity at recombinant GluA1 receptor expressed in Xenopus oocytes	[PMID: 20096591]
Oocyte	EC₅₀	0.382 μM Compound: (S)-F-Willardiine	Agonist activity at recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes Agonist activity at recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes	[PMID: 20096591]
Oocyte	EC₅₀	0.46 μM Compound: (S)-2b	Agonist activity at cyclothiazide-desensitized rat recombinant flip iGluR2(Q) expressed in Xenopus laevis oocytes by two electrode voltage-clamp electrophysiology method Agonist activity at cyclothiazide-desensitized rat recombinant flip iGluR2(Q) expressed in Xenopus laevis oocytes by two electrode voltage-clamp electrophysiology method	[PMID: 18811139]
Oocyte	EC₅₀	0.463 μM Compound: (S)-F-Willardiine	Agonist activity at recombinant GluA2 receptor flip isoform expressed in Xenopus oocytes Agonist activity at recombinant GluA2 receptor flip isoform expressed in Xenopus oocytes	[PMID: 20096591]
Oocyte	EC₅₀	11.9 μM Compound: (S)-2b	Agonist activity at cyclothiazide-desensitized rat recombinant flip iGluR4 expressed in Xenopus laevis oocytes by two electrode voltage-clamp electrophysiology method Agonist activity at cyclothiazide-desensitized rat recombinant flip iGluR4 expressed in Xenopus laevis oocytes by two electrode voltage-clamp electrophysiology method	[PMID: 18811139]
Oocyte	EC₅₀	11.9 μM Compound: (S)-F-Willardiine	Agonist activity at recombinant GluA4 receptor flip isoform expressed in Xenopus oocytes Agonist activity at recombinant GluA4 receptor flip isoform expressed in Xenopus oocytes	[PMID: 20096591]
Oocyte	EC₅₀	20.9 μM Compound: (S)-2b	Agonist activity at cyclothiazide-desensitized rat recombinant flip iGluR3 expressed in Xenopus laevis oocytes by two electrode voltage-clamp electrophysiology method Agonist activity at cyclothiazide-desensitized rat recombinant flip iGluR3 expressed in Xenopus laevis oocytes by two electrode voltage-clamp electrophysiology method	[PMID: 18811139]
Oocyte	EC₅₀	20.9 μM Compound: (S)-F-Willardiine	Agonist activity at recombinant GluA3 receptor expressed in Xenopus oocytes Agonist activity at recombinant GluA3 receptor expressed in Xenopus oocytes	[PMID: 20096591]
Oocyte	EC₅₀	20.9 μM Compound: (S)-F-Willardiine	Agonist activity at recombinant GluA3 receptor flip isoform expressed in Xenopus oocytes Agonist activity at recombinant GluA3 receptor flip isoform expressed in Xenopus oocytes	[PMID: 20096591]

In Vitro

(S)-(-)-5-Fluorowillardiine (10-100 μM; 24 h) 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) 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) binds to mouse GluK5 kainate receptor subunits expressed in Sf9 cell membranes with a K_i 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

CAS No. 140187-23-1
Masse moléculaire 217.15
Formule C₇H₈FN₃O₄
SMILES

OC([C@@H](N)CN1C=C(F)C(NC1=O)=O)=O
Synonyms

(5S)-Fluorowillardiine; (S)-5-Fluorowillardiine
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Calculators

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight Molecular Weight

Calculateur de dilution

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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