(S)-(-)-5-Iodowillardiine

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Description: Highly potent and subtype-selective kainate agonist
Purity: ≥98% (HPLC)
Datasheet
Citations (2)
Reviews
Literature (3)

Biological Activity for (S)-(-)-5-Iodowillardiine

Demonstrates high affinity for the kainate receptor subtype hGluK1 (formerly hGluR5) (Ki = 0.24 nM) and 600-4000-fold selectivity over both the AMPA receptor subtypes and the homomeric kainate receptor hGluK2 (formerly hGluR6).

Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.

Technical Data for (S)-(-)-5-Iodowillardiine

M. Wt 325.06
Formula C7H8IN3O4
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 140187-25-3
PubChem ID 447196
InChI Key AXXYLTBQIQBTES-BYPYZUCNSA-N
Smiles O=C(N1)N(C[C@]([H])(N)C(O)=O)C=C(I)C1=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for (S)-(-)-5-Iodowillardiine

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
1.1eq. NaOH 8.12 25

Preparing Stock Solutions for (S)-(-)-5-Iodowillardiine

The following data is based on the product molecular weight 325.06. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.25 mM 12.31 mL 61.53 mL 123.05 mL
1.25 mM 2.46 mL 12.31 mL 24.61 mL
2.5 mM 1.23 mL 6.15 mL 12.31 mL
12.5 mM 0.25 mL 1.23 mL 2.46 mL

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Product Datasheets for (S)-(-)-5-Iodowillardiine

Certificate of Analysis / Product Datasheet
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References for (S)-(-)-5-Iodowillardiine

References are publications that support the biological activity of the product.

Jane et al (1997) Synthesis of willardiine and 6-azawillardiine analogs: pharmacological characterization on cloned homomeric human AMPA and kainate receptor subtypes. J.Med.Chem. 40 3645 PMID: 9357531

Patneau et al (1992) Activation and desensitization of AMPA/kainate receptors by novel derivatives of willardiine. J.Neurosci. 12 595 PMID: 1371315

Swanson et al (1998) Kainate receptors exhibit differential sensitivities to (S)-5-iodowillardiine. Mol.Pharmacol. 53 942 PMID: 9584222

Wong et al (1994) Willardiines differentiate agonist binding sites for kainate-versus AMPA-preferring glutamate receptors in DRG and hippocampal neurones. J.Neurosci. 14 3881 PMID: 7515954

Thompson et al (1996) Depolarising effects of certain derivatives of (S) willardiine upon in vitro neonatal rat dorsal roots. Br.J.Pharmacol. 117 331P


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Keywords: (S)-(-)-5-Iodowillardiine, (S)-(-)-5-Iodowillardiine supplier, potent, subtype, selective, kainate, agonists, Glutamate, Kainate, Receptors, iGluR, Ionotropic, GluR5, GluK1, 0307, Tocris Bioscience

2 Citations for (S)-(-)-5-Iodowillardiine

Citations are publications that use Tocris products. Selected citations for (S)-(-)-5-Iodowillardiine include:

Pansiot et al (2010) Neuroprotective effect of inhaled nitric oxide on excitotoxic-induced brain damage in neonatal rat. Proc Natl Acad Sci U S A 5 e10916 PMID: 20532231

Pollok and Reiner (2020) Subunit-selective iGluR antagonists can potentiate heteromeric receptor responses by blocking desensitization. Proc Natl Acad Sci U S A 117 25851 PMID: 32999066


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Literature in this Area

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