1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. nAChR
  3. TC-2559 difumarate

TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect.

For research use only. We do not sell to patients.

TC-2559 difumarate Chemical Structure

TC-2559 difumarate Chemical Structure

CAS No. : 2454492-41-0

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1 mg USD 249 In-stock
5 mg USD 620 In-stock
10 mg USD 995 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of TC-2559 difumarate:

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Description

TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect[1][2].

In Vivo

TC-2559 difumarate (1-10 mg/kg; i.p.) dose dependently reduces acute formalin-induced biphasic nociceptive responses in mice[2].
TC-2559 difumarate (0.3-3 mg/kg; i.p.) dose dependently inhibits CCI-induced neuropathic pain in rats[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Adult male mice (body weight 15-30 g) (formalin test)[2]
Dosage: 1, 3, 10 mg/kg
Administration: I.p.
Result: Dose dependently reduced both early and late phases of formalin induced nociceptive behavioral responses.
Animal Model: Adult male SD rats (body weight 200-220 g) (chronic constriction injury (CCI))[2]
Dosage: 0.3, 1, 3 mg/kg
Administration: I.p.
Result: Significantly reversed CCI induced the paw withdrawal threshold decreases.
Molecular Weight

438.43

Formula

C20H26N2O9

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CCOC1=CN=CC(/C=C/CCNC)=C1.O=C(/C=C/C(O)=O)O.O=C(/C=C/C(O)=O)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 43.84 mg/mL (99.99 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 2.2809 mL 11.4043 mL 22.8087 mL 57.0216 mL
5 mM 0.4562 mL 2.2809 mL 4.5617 mL 11.4043 mL
10 mM 0.2281 mL 1.1404 mL 2.2809 mL 5.7022 mL
15 mM 0.1521 mL 0.7603 mL 1.5206 mL 3.8014 mL
20 mM 0.1140 mL 0.5702 mL 1.1404 mL 2.8511 mL
25 mM 0.0912 mL 0.4562 mL 0.9123 mL 2.2809 mL
30 mM 0.0760 mL 0.3801 mL 0.7603 mL 1.9007 mL
40 mM 0.0570 mL 0.2851 mL 0.5702 mL 1.4255 mL
50 mM 0.0456 mL 0.2281 mL 0.4562 mL 1.1404 mL
60 mM 0.0380 mL 0.1901 mL 0.3801 mL 0.9504 mL
80 mM 0.0285 mL 0.1426 mL 0.2851 mL 0.7128 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
TC-2559 difumarate
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