Tebanicline hydrochloride|cas 203564-54-9

Cas No.:	203564-54-9
Synonyms:	Ebanicline hydrochloride; ABT594 hydrochloride; ABT-594 hydrochloride; ABT 594 hydrochloride
SMILES:	ClC(C=C1)=NC=C1OC[C@@H]2NCC2.[H]Cl
Formula:	C₉H₁₂Cl₂N₂O
M.Wt:	235.11
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

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 oocytesTebanicline 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. 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. 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.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC47771	PNU-282987	PNU-282987 is a novel selective agonist of the alpha7 nAChR with Ki of 26 nM for rat alpha7 nAChR. PNU-282987 shows no activity at all tested monoamine, muscarine, glutamate, and GABA receptors, except 5-HT3 receptors with Ki of 930 nM.
DC47556	nAChR agonist 2	nAChR agonist 2 (compound 8) is a selective alpha4beta2 (α4β2) nAChR agonist (Kd=26 nM).
DC47555	CP-601932	CP-601932 ((1S,5R)-CP-601927) is a high-affinity partial agonist at α3β4 nAChR (EC50=~ 3 μM). CP-601932 has the same high-binding affinity at α3β4 (Ki=21 nM) as at α4β2 nAChRs (Ki=21 nM) and an order of magnitude lower affinity for α6 and α7 nAChR subtypes. CP-601932 selectively decreases ethanol but not sucrose consumption and operant self-administration following long-term exposure. CP-601932 readily penetrates the CNS.
DC47554	Anabaseine	Anabaseine, an alkaloid, stimulates a wide variety of animal nicotinic acetylcholine receptors (AChRs), especially the neuromuscular receptors and α7 AChRs.
DC47050	Simpinicline	Simpinicline (OC-02), a highly selective nicotinic acetylcholine receptor (nAChR) agonist, shows potent antiviral activity against the SARS-CoV-2 variants in cell culture with an IC50 of 0.04 µM.
DC47049	Ropanicant	Ropanicant (SUVN-911 free base) is a novel, potent, selective, and orally active neuronal nicotinic acetylcholine α4β2 receptor antagonist for the research of depression.
DC46863	Epiboxidine	Epiboxidine is a potent and selective neural nAChR agonist with Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. Epiboxidine is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418.
DC46640	Sulfoxaflor	Sulfoxaflor is a sulfoximine insecticide and is an agonist of nAChR1 and nAChR2 subtypes. Sulfoxaflor is used for the control of sap-feeding insects such as Myzus persicae, Aphis gossypii, Bemissia tabaci and Nilaparvata lugens.
DC46496	TQS	TQS is a α7 nicotinic acetylcholine receptor (nAChR) positive allosteric modulator. TQS can be used for the research of neuroinflammatory pain.
DC46387	α-Conotoxin Vc1.1 TFA	α-Conotoxin Vc1.1 TFA is a disulfide-bonded peptide isolated from Conus victoriae and is a selective nAChR antagonist. α-Conotoxin Vc1.1 TFA inhibits α3α5β2, α3β2 and α3β4 with IC50s of 7.2 μM, 7.3 μM and 4.2 μM, respectively, and has less inhibitory effect on other nAChR subtypes. α-Conotoxin Vc1.1 TFA has the potential for neuropathic pain reserach.