Description: Positive allosteric modulator of α7 nAChR; active in vivo
Chemical Name:N-(5-Chloro-2,4-dimethoxyphenyl)-N'-(5-methyl-3-isoxazolyl)-urea
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Positive allosteric modulator of α7 neuronal nicotinic acetylcholine receptors (EC50 = 216 nM), with no detectable effect on α4β2, α3β4 and α9α10 receptors. Active in vivo following systemic administration. Neuroprotective in an in vivo model of transient focal cerebral ischemia.
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Technical Data
M. Wt
311.72
Formula
C13H14ClN3O4
Storage
Desiccate at +4°C
Purity
≥99% (HPLC)
CAS Number
501925-31-1
PubChem ID
311434
InChI Key
CEIIEALEIHQDBX-UHFFFAOYSA-N
Smiles
COC1=CC(OC)=C(Cl)C=C1NC(=O)NC1=NOC(C)=C1
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
31.17
100
Preparing Stock Solutions
The following data is based on the product molecular weight 311.72. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
3.21 mL
16.04 mL
32.08 mL
5 mM
0.64 mL
3.21 mL
6.42 mL
10 mM
0.32 mL
1.6 mL
3.21 mL
50 mM
0.06 mL
0.32 mL
0.64 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
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References
References are publications that support the products' biological activity.
Hurstet al (2005) A novel positive allosteric modulator of the α7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. J.Neurosci. 25 4396 PMID: 15858066
Timmermannet al (2007) An allosteric modulator of the α7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo. J.Pharmacol.Exp.Ther. 323 294 PMID: 17625074
Kalappaet al (2013) A positive allosteric modulator of α7 nAChRs augments neuroprotective effects of endogenous nicotinic agonists in cerebral ischemia. Br.J.Pharmacol. [Epub ahead of print] PMID: 23713819