Home >> Research Area >>Neuroscience>>Nicotinic Receptor>> TC 2559 difumarate

TC 2559 difumarate

CAS# 212332-35-9

TC 2559 difumarate

Catalog No. BCC7469----Order now to get a substantial discount!

Product Name & Size Price Stock
TC 2559 difumarate: 5mg $115 In Stock
TC 2559 difumarate: 10mg Please Inquire In Stock
TC 2559 difumarate: 20mg Please Inquire Please Inquire
TC 2559 difumarate: 50mg Please Inquire Please Inquire
TC 2559 difumarate: 100mg Please Inquire Please Inquire
TC 2559 difumarate: 200mg Please Inquire Please Inquire
TC 2559 difumarate: 500mg Please Inquire Please Inquire
TC 2559 difumarate: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of TC 2559 difumarate

Number of papers citing our products

Chemical structure

TC 2559 difumarate

3D structure

Chemical Properties of TC 2559 difumarate

Cas No. 212332-35-9 SDF Download SDF
PubChem ID 56972184 Appearance Powder
Formula C20H26N2O9 M.Wt 438.43
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in water
Chemical Name (E)-but-2-enedioic acid;(E)-4-(5-ethoxypyridin-3-yl)-N-methylbut-3-en-1-amine
SMILES CCOC1=CN=CC(=C1)C=CCCNC.C(=CC(=O)O)C(=O)O.C(=CC(=O)O)C(=O)O
Standard InChIKey GEWVPSJQGJBDLM-MYBAKCFCSA-N
Standard InChI InChI=1S/C12H18N2O.2C4H4O4/c1-3-15-12-8-11(9-14-10-12)6-4-5-7-13-2;2*5-3(6)1-2-4(7)8/h4,6,8-10,13H,3,5,7H2,1-2H3;2*1-2H,(H,5,6)(H,7,8)/b6-4+;2*2-1+
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of TC 2559 difumarate

DescriptionSubtype-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.

TC 2559 difumarate Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

TC 2559 difumarate Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of TC 2559 difumarate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2809 mL 11.4043 mL 22.8087 mL 45.6173 mL 57.0216 mL
5 mM 0.4562 mL 2.2809 mL 4.5617 mL 9.1235 mL 11.4043 mL
10 mM 0.2281 mL 1.1404 mL 2.2809 mL 4.5617 mL 5.7022 mL
50 mM 0.0456 mL 0.2281 mL 0.4562 mL 0.9123 mL 1.1404 mL
100 mM 0.0228 mL 0.114 mL 0.2281 mL 0.4562 mL 0.5702 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University
Featured Products
New Products
 

References on TC 2559 difumarate

5-I A-85380 and TC-2559 differentially activate heterologously expressed alpha4beta2 nicotinic receptors.[Pubmed:16674940]

Eur J Pharmacol. 2006 Jun 6;539(1-2):10-7.

The neuronal nicotinic acetylcholine receptor alpha4 and beta2 subunits expressed in heterologous expression systems assemble into at least two distinct subunit stoichiometries of alpha4beta2 receptor. The (alpha4)2(beta2)3 stoichiometry is about 100-fold more sensitive to acetylcholine than the (alpha4)3(beta2)2 stoichiometry. In order to investigate if agonists in general distinguish high- and low-affinity alpha4beta2 nicotinic acetylcholine receptors, we have expressed human alpha4 and beta2 nicotinic acetylcholine receptor subunits in two different expression systems. The relative amounts of alpha4beta2 nicotinic acetylcholine receptors with high- and low-affinity for acetylcholine were manipulated by (a) injecting the subunit cDNAs at different alpha:beta ratios into Xenopus oocytes and (b) by culturing HEK-293 cells stably expressing alpha4beta2 nicotinic acetylcholine receptors overnight at different temperatures. The sensitivities of the alpha4beta2 nicotinic acetylcholine receptors to the agonists acetylcholine, 5-I A-85380, and TC-2559 were investigated using the voltage-clamp technique on Xenopus oocytes and using a fluorescent imaging plate reader to measure calcium responses from HEK-293 cells. Like acetylcholine, 5-I A-85380 produced biphasic concentration-response curves and the high-affinity component became larger when the cells were manipulated to produce a greater proportion of (alpha4)2(beta2)3 nicotinic acetylcholine receptors. Interestingly, under all circumstances, TC-2559 produced monophasic concentration-response curves. In oocytes injected with alpha4 and beta2 subunits in the 1:1 ratio the maximum effect of TC-2559 was 28% of that of acetylcholine. The EC50 for TC-2559 was not changed when oocytes were manipulated to express exclusively (alpha4)2(beta2)3 nicotinic acetylcholine receptors, however, the maximum effect of TC-2559 was dramatically enhanced. These results suggest that TC-2559 is a selective agonist of the (alpha4)2(beta2)3 nicotinic acetylcholine receptor stoichiometry.

The nicotinic alpha 4 beta 2 receptor selective agonist, TC-2559, increases dopamine neuronal activity in the ventral tegmental area of rat midbrain slices.[Pubmed:12871651]

Neuropharmacology. 2003 Sep;45(3):334-44.

The ability of alpha4beta2 nicotinic acetylcholine receptors to modulate dopaminergic (DA) cell activity in the ventral tegmental area (VTA) in rat midbrain slices was assessed using a selective alpha4beta2 receptor agonist, TC-2559 ((E)-N-methyl-4-[3-(5-ethoxypyridin)y1]-3-buten-1-amine). The selectivity of TC-2559 was characterized across 6 recombinant human nicotinic receptors (alpha4beta2, alpha2beta4, alpha4beta4, alpha3beta4, alpha3beta2 and alpha7) stably expressed in mammalian cell lines. Using a fluorescent imaging plate reader and fluo-3 to monitor changes in intracellular calcium, TC-2559 was found to be at least 69 fold more potent on alpha4beta2 than on other heteromeric subtypes, with an efficacy of 33%. No activity on the homomeric alpha7 subtype was detected. TC-2559 also showed selectivity for alpha4beta2 over the alpha4beta4 and alpha7 subtypes expressed in Xenopus oocytes. When bath applied to VTA slices, TC-2559 increased the firing of DA cells in a dose-dependent manner, in the same concentration range that activates alpha4beta2 receptors in recombinant cell lines or oocytes. The effect of TC-2559 was blocked by 2 microM dihydro-beta-erythroidine (an alpha4beta2-preferring antagonist), but not by 10 nM methyllycaconitine (an alpha7 antagonist). Glutamate receptor antagonists (6-cyano-7-nitroquinoxaline-2,3-dione and D(-)-2-amino-5-phosphonopentanoic acid) did not reduce TC-2559-induced responses, suggesting that the increase in DA cell firing induced by TC-2559 is caused by direct postsynaptic depolarisation via the activation of alpha4beta2 receptors and not by enhancement of glutamate release.

TC-2559: a novel orally active ligand selective at neuronal acetylcholine receptors.[Pubmed:11099699]

Eur J Pharmacol. 2000 Dec 1;409(1):45-55.

TC-2559 [(E)-N-Methyl-4-[3-(5-ethoxypyridin)yl]-3-buten-1-amine] is a novel nicotinic agonist markedly more selective than recently reported novel nicotinic receptor ligands (selectivity ratio for central nervous system (CNS) to peripheral nervous system (PNS)>4000). TC-2559 competes effectively with [3H]-nicotine binding (K(i)=5 nM) but not with [125I]-bungarotoxin (>50,000 nM). Dopamine release from striatal synaptosomes and ion flux from thalamic synaptosomes indicate that TC-2559 is potent and efficacious in the activation of CNS receptors and significantly reduced glutamate-induced neurotoxicity in vitro. TC-2559 has no detectable effects on muscle and ganglion-type nicotinic acetylcholine receptors at concentrations up to 1 mM. TC-2559 significantly attenuates scopolamine-induced cognitive deficits in a step-through passive avoidance task. Acute and repeated oral dosing of TC-2559 enhances performance in a radial arm maze task. In contrast to the effects of equimolar concentrations of (-) nicotine, TC-2559 does not induce hypothermia and locomotor activity is not enhanced following repeated daily administration of 14 days. TC-2559 has a markedly enhanced CNS-PNS selectivity ratio and an intra-CNS selectivity as evidenced by the improved cognition without increased locomotor activity. The in vitro and in vivo studies in the present study suggest that TC-2559 has the desired profile to be further evaluated as a potential therapeutic agent for neurodegenerative diseases.

Keywords:

TC 2559 difumarate,212332-35-9,Natural Products,Nicotinic Receptor, buy TC 2559 difumarate , TC 2559 difumarate supplier , purchase TC 2559 difumarate , TC 2559 difumarate cost , TC 2559 difumarate manufacturer , order TC 2559 difumarate , high purity TC 2559 difumarate

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: