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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Based on 1 publication(s) in Google Scholar

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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.
SMILES

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

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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TC-2559 difumarate Related Classifications

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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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TC-2559 difumarate
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HY-136207
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