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

TC-2559 difumarate 

目录号: HY-136207
产品使用指南

TC-2559 difumarate 是 CNS 选择性,具有口服活性的烟碱乙酰胆碱受体 (nAChR) α4β2 亚型的部分激动剂。TC-2559 difumarate 对 α2β4、α4β4 和 α3β4 受体表现出选择性,EC50在 10-30 µM 范围内。

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TC-2559 difumarate Chemical Structure

TC-2559 difumarate Chemical Structure

CAS No. : 2454492-41-0

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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].

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.

2454492-41-0

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

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

References
  • 摩尔计算器

  • 稀释计算器

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Keywords:

TC-2559 difumaratenAChRNicotinic acetylcholine receptorsnociceptiveresponsespainCNS-selectiveoralInhibitorinhibitorinhibit

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产品名称:
TC-2559 difumarate
目录号:
HY-136207
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