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Submit ReviewNS 9283 is a positive allosteric modulator of α4β2 receptor; increases the potency of Ach-evoked currents ~60 fold without affecting 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.
NS 9283 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 248.24 |
公式 | C14H8N4O |
储存 | Store at +4°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 12.41 | 50 | |
1eq. HCl | 4.96 | 20 |
以下数据基于产品分子量 248.24。 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for NS 9283, please let us know.
关键词: NS 9283, NS 9283 supplier, NS9283, Acetylcholine, nicotinic, ⓮⓶, receptors, positive, allosteric, modulators, PAM, Nicotinic, (a4b2), Receptors, 5112, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 NS 9283 的部分引用包括:
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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