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Tebanicline hydrochloride

Tebanicline hydrochloride
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Purity:98.71%
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Tebanicline hydrochloride

Catalog No. T3720Cas No. 203564-54-9
Tebanicline hydrochloride (Ebanicline hydrochloride) , is an effective synthetic nicotinic (non-opioid) analgesic drug.
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Pack SizePriceAvailabilityQuantity
1 mg$37In Stock
2 mg$51In Stock
5 mg$91In Stock
10 mg$141In Stock
25 mg$277In Stock
50 mg$498In Stock
100 mg$725In Stock
500 mg$1,520In Stock
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Product Introduction

Bioactivity
Description
Tebanicline hydrochloride (Ebanicline hydrochloride) , is an effective synthetic nicotinic (non-opioid) analgesic drug.
Targets&IC50
nAChR:37 pM(ki)
In vitro
Tebanicline is a novel, potent cholinergic nAChR ligand with analgesic properties that shows preferential selectivity for neuronal nAChRs. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM. Functionally, tebanicline is an agonist. At the transfected human α4β2 neuronal nAChR in K177 cells, with increased 86Rb+ efflux as a measure of cation efflux, ABT-594 has an EC50 value of 140 nM with an intrinsic activitycompared with (?)-nicotine of 130%; at the nAChR subtype expressed in IMR-32 cells, an EC50 of 340 nM; at the F11 dorsal root ganglion cell line, an EC50 of 1220 nM; and via direct measurement of ion currents, an EC50 value of 56,000 nM at the human α7 homo-oligimeric nAChR produced in oocytes[1]
In vivo
Tebanicline is a potent antinociceptive agent with full efficacy in models of acute and persistent pain and that these effects are mediated predominately by an action at central neuronal nAChRs[2]. Tebanicline produces significant antinociceptive effects in mice against both acute noxious thermal stimulation. ABT-594 is orally active, but 10-fold less potent by this route than after i.p. administration. The antinociceptive effect of ABT-594 is prevented, but not reversed, by the noncompetitive neuronal nicotinic acetylcholine receptor antagonist[3]. Tebanicline has antinociceptive effects in rat models of acute thermal, persistent chemical, and neuropathic pain. Direct injection of tebanicline into the nucleus raphe magnus (NRM) is antinociceptive in a thermal threshold test and destruction of serotonergic neurons in the NRM attenuates the effect of systemic tebanicline[4].
AliasABT-594 hydrochloride, Ebanicline hydrochloride
Chemical Properties
Molecular Weight235.11
FormulaC9H12Cl2N2O
Cas No.203564-54-9
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (212.67 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM4.2533 mL21.2666 mL42.5333 mL212.6664 mL
5 mM0.8507 mL4.2533 mL8.5067 mL42.5333 mL
10 mM0.4253 mL2.1267 mL4.2533 mL21.2666 mL
20 mM0.2127 mL1.0633 mL2.1267 mL10.6333 mL
50 mM0.0851 mL0.4253 mL0.8507 mL4.2533 mL
100 mM0.0425 mL0.2127 mL0.4253 mL2.1267 mL

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