[CAS NO. 1026134-63-3] Nelonicline

Name: Nelonicline
Brand: Arctom Scientific
SKU: AS939322

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PRODUCTS SPECIFICATIONS [1026134-63-3]

Distributor

Catalog

AS939322

Brand

Arctom Scientific

CAS

1026134-63-3

DESCRIPTION [1026134-63-3]

Overview

MDL	MFCD27987904
Molecular Weight	313.42
Molecular Formula	C17H19N3OS
SMILES	[C@@H]1([C@H]2C[C@H](C3)C[C@@H]1C[N@]3C2)OC4=NN=C(C5=CC=CC=C5)S4

For research use only. We do not sell to patients.

Summary

Nelonicline (ABT-126) is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain ( K _i =12.3 nM). Nelonicline is used for the research of shizophrenia and Alzheimer's disease ^[1] ^[2] ^[3] .

IC50 & Target

Neuronal nicotinic receptor ^[1]

In Vitro

Nelonicline is an agonist that binds with high affinity to α7 nAChRs in human brain (K _i = 12.3 nM) and activates currents in Xenopus oocytes expressing recombinant human α7 nAChRs (EC ₅₀ =2 μM; intrinsic activity of 74% relative to acetylcholine). Nelonicline does bind to α3β4* nAChRs in human IMR-32 neuroblastoma cells (K _i =60 nM), but has only 12% efficacy at 100,000 nM in a calcium flux assay in these cell. Like some other α7 nAChR agonists, Nelonicline is also a 5-HT3 receptor antagonist, but it has >10-fold lower affinity for this receptor than for α7 nAChRs (K _i of 140 nM) ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01676935	AbbVie (prior sponsor, Abbott)\|AbbVie	Alzheimer´s Disease	August 2012	Phase 2
NCT00867399	Abbott	Alzheimer´s Disease	March 2009	Phase 1
NCT01095562	AbbVie (prior sponsor, Abbott)\|AbbVie	Cognitive Deficits in Schizophrenia	March 2010	Phase 2
NCT01690195	AbbVie (prior sponsor, Abbott)\|AbbVie	Alzheimer´s Disease	September 2012	Phase 2
NCT01527916	AbbVie (prior sponsor, Abbott)\|AbbVie	Alzheimer´s Disease	February 2012	Phase 2
NCT00912431	Abbott	Healthy	June 2009	Phase 1
NCT01678755	AbbVie (prior sponsor, Abbott)\|AbbVie	Schizophrenia	August 2012	Phase 2
NCT01482845	Abbott	Alzheimer´s Disease	November 2011	Phase 1
NCT01834638	AbbVie	Schizophrenia	March 2013	Phase 2
NCT01043458	Abbott	Schizophrenia	November 2009	Phase 1
NCT01549834	AbbVie (prior sponsor, Abbott)\|AbbVie	Alzheimer´s Disease	March 2012	Phase 2
NCT00959634	Abbott	Healthy Volunteers	August 2009	Phase 1
NCT01655680	AbbVie (prior sponsor, Abbott)\|AbbVie	Schizophrenia	May 2012	Phase 2
NCT00948909	AbbVie (prior sponsor, Abbott)\|AbbVie	Alzheimer´s Disease	October 2009	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 12.5 mg/mL ( 39.88 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.1906 mL	15.9530 mL	31.9061 mL
5 mM	0.6381 mL	3.1906 mL	6.3812 mL
10 mM	0.3191 mL	1.5953 mL	3.1906 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 1.25 mg/mL (3.99 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1.25 mg/mL (3.99 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 1.25 mg/mL (3.99 mM); Clear solution

* All of the co-solvents are available by MCE.