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(S) -Willardiine

CAT: 0804-HY-12499-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-12499-01Size:5 mg
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Description
(S) -Willardiine is a potent agonist of AMPA/kainate receptors with EC50 of 44.8 uM. IC50 value: 44.8 uM (EC50) [1] Target: AMPA/kainate receptor agonist in vitro: The (S) - but not (R) -isomers of willardiine and 5-bromowillardiine were potent agonists, producing rapidly but incompletely desensitizing responses [1]. At a concentration of 1.8 mM, Ca2+ inhibited the currents induced by 100 microM willardiine by approximately 50% [2]. in vivo: In newborn mice (P5, histopathology at P10), local injection of the AMPA receptor agonist S-bromo-willardiine at day 5 after birth induced cortical damage and white matter damage, which was reduced in a dose-dependent manner by the AMPA receptor antagonists [3].
CAS Number
21416-43-3
Product Name Alternative
(-) -Willardiine
UNSPSC
12352005
Hazard Statement
H302, H312, H332
Target
IGluR
Type
Reference compound
Related Pathways
Membrane Transporter/Ion Channel; Neuronal Signaling
Applications
Neuroscience-Neuromodulation
Field of Research
Neurological Disease
Assay Protocol
https://www.medchemexpress.com/_S_-Willardiine.html
Purity
98.93
Solubility
H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
N[C@@H](CN(C(N1)=O)C=CC1=O)C(O)=O
Molecular Formula
C7H9N3O4
Molecular Weight
199.17
Precautions
H302, H312, H332
References & Citations
[1]Patneau DK, et al. Activation and desensitization of AMPA/kainate receptors by novel derivatives of willardiine. J Neurosci. 1992 Feb;12 (2) :595-606.|[2]Fukushima T, et al. Calcium inhibits willardiine-induced responses in kainate receptor GluR6 (Q) /KA-2. Neuroreport. 2001 Jan 22;12 (1) :163-7.|[3]Gressens P, et al. The effects of AMPA receptor antagonists in models of stroke and neurodegeneration. Eur J Pharmacol. 2005 Sep 5;519 (1-2) :58-67.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
AMPA Receptor; Kainate Receptor