| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
TC 2559 targets the α4β2 subunit-containing nicotinic acetylcholine receptors (nAChRs). It is a partial agonist at these receptors with an EC50 value of 0.18 µM for calcium signaling in HEK293 cells expressing human recombinant nAChRs. It is selective for α4β2 over α2β4, α4β4, α3β4, α3β2, and α7 subunit-containing nAChRs.
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| ln Vitro |
In vitro, TC 2559 is a potent agonist at α4β2 nAChRs with an EC50 of 0.18 µM for calcium signaling. It is selective for α4β2 over other nAChR subtypes, with EC50 values of 14, 12.5, >30, >100, and >100 µM for α2β4, α4β4, α3β4, α3β2, and α7 receptors, respectively. It increases dopamine cell firing in the rat ventral tegmental area (VTA) in vitro.
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| ln Vivo |
TC 2559 increases spontaneous inhibitory postsynaptic currents (sIPSCs) in dorsal horn neurons, indicating an enhancement of inhibitory synaptic transmission, an effect that is blocked by the α4β2 subunit-containing nAChR antagonist DHβE. It reduces formalin-induced pain behaviors in animal models. The compound's ability to enhance inhibitory neurotransmission contributes to its analgesic effects.
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| Enzyme Assay |
In vitro receptor binding and functional assays for TC 2559 involve measuring calcium signaling in cells expressing human recombinant nAChRs. Cells are loaded with a calcium-sensitive fluorescent indicator and treated with varying concentrations of TC 2559. Receptor activation is measured as changes in fluorescence intensity. EC50 values are calculated from concentration-response curves.
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| Cell Assay |
For in vitro cell-based assays, HEK293 cells expressing human recombinant nAChR subtypes are cultured and treated with TC 2559 at various concentrations. Calcium signaling is measured using fluorescent indicators. Dopamine cell firing is measured in rat ventral tegmental area (VTA) slices using electrophysiological recording. Spontaneous inhibitory postsynaptic currents (sIPSCs) are recorded in dorsal horn neurons.
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| Animal Protocol |
In vivo animal studies for TC 2559 typically use rodent models of pain. The compound is administered systemically, and pain behaviors are assessed using the formalin test or other pain models. Electrophysiological recordings may be performed to measure the effects on inhibitory synaptic transmission in spinal cord neurons. Specific dosing regimens and detailed protocols are not extensively provided in the available literature.
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| ADME/Pharmacokinetics |
TC 2559 (fumarate) has a molecular formula of C12H18N2O • 2C4H4O4 and a molecular weight of 438.43. It is a solid and is slightly soluble in DMSO and methanol. It should be stored at -20°C. The compound is for research use only. Detailed pharmacokinetic parameters are not extensively characterized in the available literature.
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| Toxicity/Toxicokinetics |
Specific toxicity data for TC 2559 are not extensively provided in the available literature. As a nAChR agonist, it would be expected to have a safety profile related to modulation of cholinergic signaling. The compound is for research use only and is not for human or clinical use. Standard toxicology assessments would be required for therapeutic development.
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| References | |
| Additional Infomation |
TC 2559 is a CNS-selective partial agonist for α4β2 subunit-containing nicotinic acetylcholine receptors (nAChRs). It is selective for α4β2 over other nAChR subtypes. The compound increases dopamine cell firing and enhances inhibitory synaptic transmission. It reduces formalin-induced pain and has been studied for its potential in pain management. No approved therapeutic status is reported.
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| Molecular Formula |
C20H26N2O9
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|---|---|
| Molecular Weight |
438.428446292877
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| Exact Mass |
438.164
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| CAS # |
212332-35-9
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| Related CAS # |
TC-2559 difumarate;2454492-41-0
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| PubChem CID |
56972184
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
1.917
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
31
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| Complexity |
301
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(CC)C1=CN=CC(=C1)C=CCCNC.OC(C=CC(=O)O)=O.OC(C=CC(=O)O)=O
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| InChi Key |
GEWVPSJQGJBDLM-MYBAKCFCSA-N
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| InChi Code |
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+
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| Chemical Name |
(E)-but-2-enedioic acid;(E)-4-(5-ethoxypyridin-3-yl)-N-methylbut-3-en-1-amine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2809 mL | 11.4043 mL | 22.8087 mL | |
| 5 mM | 0.4562 mL | 2.2809 mL | 4.5617 mL | |
| 10 mM | 0.2281 mL | 1.1404 mL | 2.2809 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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