Description: Positive allosteric modulator of α4β2
Chemical Name: 3-[3-(3-Pyridinyl)-1,2,4-oxadiazol-5-yl]benzonitrile
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Positive allosteric modulator of α4β2 receptor; increases the potency of Ach-evoked currents ~60 fold without effecting the maximum efficacy (HEK293-hα4β2 cells). Reduces the rate of recovery from desensitization and slows the rate of deactivation. Displays a synergistic effect on the Emax when given with NS206 at 3α:2β receptors.
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Technical Data
M. Wt
248.24
Formula
C14H8N4O
Storage
Store at +4°C
Purity
≥99% (HPLC)
CAS Number
913830-15-6
PubChem ID
11998180
InChI Key
HGFXDSQLRSWUBO-UHFFFAOYSA-N
Smiles
N#CC1=CC(C2=NC(C3=CN=CC=C3)=NO2)=CC=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
1eq. HCl
4.96
20
DMSO
12.41
50
Preparing Stock Solutions
The following data is based on the product molecular weight 248.24. 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
4.03 mL
20.14 mL
40.28 mL
5 mM
0.81 mL
4.03 mL
8.06 mL
10 mM
0.4 mL
2.01 mL
4.03 mL
50 mM
0.08 mL
0.4 mL
0.81 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Grupeet al (2013) Unravelling the mechanism of action of NS9283, a positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors. Br.J.Pharmacol. 168 2000 PMID: 23278456
Mohleret al (2014) Discriminative-stimulus effects of NS9283, a nicotinic α4β2* positive allosteric modulator, in nicotine-discriminating rats. Psychopharmacology (Berl). 231 67 PMID: 23925734
Olsenet al (2013) Two distinct allosteric binding sites at α4β2 nicotinic acetylcholine receptors revealed by NS206 and NS9283 give unique insights to binding activity-associated linkage at Cys-loop receptor J.Biol.Chem. 288 35997 PMID: 24169695