Molecular structure of TC 2559 difumarate, CAS Number: 212332-35-9
TC 2559 difumarate (CAS 212332-35-9)
Alternate Names:
4-(5-ethoxy-3-pyridinyl)-N-methyl-(3E)-3-buten-1-amine difumarate
Application:
TC 2559 difumarate is a partial agonist for AChR α4β2
CAS Number:
212332-35-9
Purity:
>98%
Molecular Weight:
438.43
Molecular Formula:
C12H18N2O•2C4H4O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
TC 2559 difumarate is a subtype-selective partial agonist for AChR α4β2 (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). It displays selectivity for (α4)2(β2)3 receptor stoichiometry and enhanced CNS-PNS slectivity ratio.
TC 2559 difumarate (CAS 212332-35-9) References
- Stable expression and functional characterization of a human nicotinic acetylcholine receptor with α6β2 properties: discovery of selective antagonists. | Capelli, AM., et al. 2011. Br J Pharmacol. 163: 313-29. PMID: 21232042
- Non-equivalent ligand selectivity of agonist sites in (α4β2)2α4 nicotinic acetylcholine receptors: a key determinant of agonist efficacy. | Mazzaferro, S., et al. 2014. J Biol Chem. 289: 21795-806. PMID: 24936069
- Peripheral alpha4beta2 nicotinic acetylcholine receptor signalling attenuates tactile allodynia and thermal hyperalgesia after nerve injury in mice. | Saika, F., et al. 2015. Acta Physiol (Oxf). 213: 462-71. PMID: 25491757
- TC-2559, an α4β2 nicotinic acetylcholine receptor agonist, suppresses the expression of CCL3 and IL-1β through STAT3 inhibition in cultured murine macrophages. | Kiguchi, N., et al. 2015. J Pharmacol Sci. 128: 83-6. PMID: 26012743
- α4β2 Nicotinic Acetylcholine Receptors: RELATIONSHIPS BETWEEN SUBUNIT STOICHIOMETRY AND FUNCTION AT THE SINGLE CHANNEL LEVEL. | Mazzaferro, S., et al. 2017. J Biol Chem. 292: 2729-2740. PMID: 28031459
- MeCP2-deficient mice have reduced α4 and α6 nicotinic receptor mRNA and altered behavioral response to nicotinic agonists. | Leung, J., et al. 2017. Behav Brain Res. 330: 118-126. PMID: 28506623
- Inhibition of peripheral macrophages by nicotinic acetylcholine receptor agonists suppresses spinal microglial activation and neuropathic pain in mice with peripheral nerve injury. | Kiguchi, N., et al. 2018. J Neuroinflammation. 15: 96. PMID: 29587798
- Inflammatory Macrophages in the Sciatic Nerves Facilitate Neuropathic Pain Associated with Type 2 Diabetes Mellitus. | Saika, F., et al. 2019. J Pharmacol Exp Ther. 368: 535-544. PMID: 30602591
- Insights Into the Differential Desensitization of α4β2 Nicotinic Acetylcholine Receptor Isoforms Obtained With Positive Allosteric Modulation of Mutant Receptors. | Papke, RL. and Stokes, C. 2023. Mol Pharmacol. 103: 63-76. PMID: 36414373
Inhibitor of:
AChRγ.Activator of:
AChR α 4, AChRγ, AChRbeta2, and mAChR M4.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
TC 2559 difumarate, 10 mg | sc-203707 | 10 mg | $185.00 | |||
TC 2559 difumarate, 50 mg | sc-203707A | 50 mg | $781.00 |