NS 9283

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Cat.No. 5112 - NS 9283 | C14H8N4O | CAS No. 913830-15-6
Description: Positive allosteric modulator of α4β2 nAChRs
Chemical Name: 3-[3-(3-Pyridinyl)-1,2,4-oxadiazol-5-yl]benzonitrile
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Reviews
Literature

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.

Compound Libraries

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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
0.5 mM 8.06 mL 40.28 mL 80.57 mL
2.5 mM 1.61 mL 8.06 mL 16.11 mL
5 mM 0.81 mL 4.03 mL 8.06 mL
25 mM 0.16 mL 0.81 mL 1.61 mL

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References

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

Grupe et 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

Mohler et al (2014) Discriminative-stimulus effects of NS9283, a nicotinic α4β2* positive allosteric modulator, in nicotine-discriminating rats. Psychopharmacology (Berl). 231 67 PMID: 23925734

Olsen et 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


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Keywords: NS 9283, NS 9283 supplier, NS9283, Acetylcholine, nicotinic, ⓮⓶, receptors, positive, allosteric, modulators, Nicotinic, (a4b2), Receptors, 5112, Tocris Bioscience

1 Citation for NS 9283

Citations are publications that use Tocris products. Selected citations for NS 9283 include:

Wang et al (2017) Unraveling amino acid residues critical for allosteric potentiation of (α4)3(β2)2-type nicotinic acetylcholine receptor responses. J.Med.Chem. 292 9988 PMID: 28446611


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

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