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.
Product information
CAS Number: 2454492-41-0
Molecular Weight: 438.43
Formula: C20H26N2O9
Chemical Name: bis((2E)-but-2-enedioic acid); [(3E)-4-(5-ethoxypyridin-3-yl)but-3-en-1-yl](methyl)amine
Smiles: CCOC1C=C(/C=C/CCNC)C=NC=1.OC(=O)/C=C/C(O)=O.OC(=O)/C=C/C(O)=O
InChiKey: GEWVPSJQGJBDLM-MYBAKCFCSA-N
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+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vivo:
TC-2559 difumarate (1-10 mg/kg; i.p.) dose dependently reduces acute formalin-induced biphasic nociceptive responses in mice. TC-2559 difumarate (0.3-3 mg/kg; i.p.) dose dependently inhibits CCI-induced neuropathic pain in rats.
References:
- Bencherif M, et al. TC-2559: a novel orally active ligand selective at neuronal acetylcholine receptors. Eur J Pharmacol. 2000;409(1):45-55.
- Cheng LZ, et al. Enhanced inhibitory synaptic transmission in the spinal dorsal horn mediates antinociceptive effects of TC-2559. Mol Pain. 2011;7:56. Published 2011 Aug 4.
Products are for research use only. Not for human use.
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