NS9283
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MedKoo CAT#: 532373

CAS#: 913830-15-6

Description: NS9283 is a positive allosteric modulator of α4β2 receptor. NS9283 increases the potency of Ach-evoked currents ~60 fold without effecting the maximum efficacy (HEK293-hα4β2 cells). It reduces the rate of recovery from desensitization and slows the rate of deactivation.


Price and Availability

Size Price Shipping out time Quantity
10mg USD 330 2 Weeks
25mg USD 630 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-30. Prices are subject to change without notice.

NS9283, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 532373
Name: NS9283
CAS#: 913830-15-6
Chemical Formula: C14H8N4O
Exact Mass: 248.0698
Molecular Weight: 248.25
Elemental Analysis: C, 67.74; H, 3.25; N, 22.57; O, 6.44


Synonym: NS9283; NS 9283; NS-9283.

IUPAC/Chemical Name: 3-[3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl]benzonitrile

InChi Key: HGFXDSQLRSWUBO-UHFFFAOYSA-N

InChi Code: InChI=1S/C14H8N4O/c15-8-10-3-1-4-11(7-10)14-17-13(18-19-14)12-5-2-6-16-9-12/h1-7,9H

SMILES Code: N#CC1=CC=CC(C2=NC(C3=CC=CN=C3)=NO2)=C1


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


References

1: Maurer JJ, Sandager-Nielsen K, Schmidt HD. Attenuation of nicotine taking and seeking in rats by the stoichiometry-selective alpha4beta2 nicotinic acetylcholine receptor positive allosteric modulator NS9283. Psychopharmacology (Berl). 2017 Feb;234(3):475-484. doi: 10.1007/s00213-016-4475-7. Epub 2016 Nov 14. PubMed PMID: 27844094.

2: Olsen JA, Ahring PK, Kastrup JS, Gajhede M, Balle T. Structural and functional studies of the modulator NS9283 reveal agonist-like mechanism of action at α4β2 nicotinic acetylcholine receptors. J Biol Chem. 2014 Sep 5;289(36):24911-21. doi: 10.1074/jbc.M114.568097. Epub 2014 Jun 30. PubMed PMID: 24982426; PubMed Central PMCID: PMC4155659.

3: Grupe M, Grunnet M, Laursen B, Bastlund JF. Neuropharmacological modulation of the P3-like event-related potential in a rat two-tone auditory discrimination task with modafinil and NS9283, a positive allosteric modulator of α4β2 nAChRs. Neuropharmacology. 2014 Apr;79:444-55. doi: 10.1016/j.neuropharm.2013.12.008. Epub 2013 Dec 17. PubMed PMID: 24361451.

4: Olsen JA, Kastrup JS, Peters D, Gajhede M, Balle T, Ahring PK. 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 receptors. J Biol Chem. 2013 Dec 13;288(50):35997-6006. doi: 10.1074/jbc.M113.498618. Epub 2013 Oct 29. PubMed PMID: 24169695; PubMed Central PMCID: PMC3861648.

5: Mohler EG, Franklin SR, Rueter LE. Discriminative-stimulus effects of NS9283, a nicotinic α4β2* positive allosteric modulator, in nicotine-discriminating rats. Psychopharmacology (Berl). 2014 Jan;231(1):67-74. doi: 10.1007/s00213-013-3207-5. Epub 2013 Aug 8. PubMed PMID: 23925734.

6: Grupe M, Jensen AA, Ahring PK, Christensen JK, Grunnet M. Unravelling the mechanism of action of NS9283, a positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors. Br J Pharmacol. 2013 Apr;168(8):2000-10. doi: 10.1111/bph.12095. PubMed PMID: 23278456; PubMed Central PMCID: PMC3623068.

7: Timmermann DB, Sandager-Nielsen K, Dyhring T, Smith M, Jacobsen AM, Nielsen EØ, Grunnet M, Christensen JK, Peters D, Kohlhaas K, Olsen GM, Ahring PK. Augmentation of cognitive function by NS9283, a stoichiometry-dependent positive allosteric modulator of α2- and α4-containing nicotinic acetylcholine receptors. Br J Pharmacol. 2012 Sep;167(1):164-82. doi: 10.1111/j.1476-5381.2012.01989.x. PubMed PMID: 22506660; PubMed Central PMCID: PMC3448921.