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Submit ReviewTC 2559 difumarate is a subtype-selective partial agonist for α4β2 nicotinic acetylcholine receptors (EC50 values are 0.18, 12.5, 14.0, > 30, > 100 and > 100 μM for α4β2, α4β4, α2β4, α3β4, α3β2 and α7 receptor subtypes respectively). Displays selectivity for (α4)2(β2)3 receptor stoichiometry and enhanced CNS-PNS selectivity ratio. Attenuates scopolamine-induced cognitive deficits in a step-through passive avoidance task.
分子量 | 438.43 |
公式 | C12H18N2O.2C4H4O4 |
储存 | Desiccate at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 2454492-41-0 |
PubChem ID | 56972184 |
InChI Key | GEWVPSJQGJBDLM-MYBAKCFCSA-N |
Smiles | CCOC1=CN=CC(/C=C/CCNC)=C1.O=C(O)/C=C/C(O)=O.O=C(O)/C=C/C(O)=O |
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 | |||
water | 43.84 | 100 |
以下数据基于产品分子量 438.43。 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 |
---|---|---|---|
1 mM | 2.28 mL | 11.4 mL | 22.81 mL |
5 mM | 0.46 mL | 2.28 mL | 4.56 mL |
10 mM | 0.23 mL | 1.14 mL | 2.28 mL |
50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
参考文献是支持产品生物活性的出版物。
Bencherif et al (2000) TC-2559: a novel orally active ligand selective at neuronal acetylcholine receptors. Eur.J.Pharmacol. 409 45 PMID: 11099699
Chen et al (2003) The nicotinic α4β2 receptor selective agonist, TC-2559, increases DA neuronal activity in the ventral tegmental area of rat midbrain slices. Neuropharmacology 45 334 PMID: 12871651
Zwart et al (2006) 5-I A-85380 and TC-2559 differentially activate heterologously expressed α4β2 nicotinic receptors. Eur.J.Pharmacol. 539 10 PMID: 16674940
If you know of a relevant reference for TC 2559 difumarate, please let us know.
关键词: TC 2559 difumarate, TC 2559 difumarate supplier, Selective, partial, agonists, α4β2, alpha4beta2, receptors, Nicotinic, Receptors, Acetylcholine, nAChR, TC2559, difumarate, 212332-35-9, (a4b2), 2737, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 TC 2559 difumarate 的部分引用包括:
Kiguchi (2018) Inhibition of peripheral macrophages by nicotinic acetylcholine receptor agonists suppresses spinal microglial activation and neuropathic pain in mice with peripheral nerve injury. J Neuroinflammation 15 96 PMID: 29587798
Sun et al (2009) Rosiglitazone inhibits alpha4 nicotinic acetylcholine receptor expression in human lung carcinoma cells through peroxisome proliferator-activated receptor gamma-independent signals. Mol Cancer Ther 8 110 PMID: 19139119
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