Nelonicline (Synonyms: ABT-126)

Name: Nelonicline
Brand: MedChemExpress
SKU: HY-16748
Rating: 4.5 (1 reviews)

Cat. No.: HY-16748 Purity: 99.82%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

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

Nelonicline Chemical Structure

CAS No. : 1026134-63-3

Size	Price	Stock	Quantity
1 mg	USD 340	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 850	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1300	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 2650	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 4250	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 6800	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
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Based on 1 publication(s) in Google Scholar

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Protocol
Purity & Documentation
References
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Description

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 (EC₅₀=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].

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

Clinical Trial

Molecular Weight

313.42

Formula

C₁₇H₁₉N₃OS

CAS No.

1026134-63-3

Appearance

Solid

Color

White to off-white

SMILES

[C@@H]1([C@H]2C[C@H](C3)C[C@@H]1C[N@]3C2)OC4=NN=C(C5=CC=CC=C5)S4

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.25 mg/mL (3.99 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.82%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (249 KB) RP-HPLC (286 KB)

Handling Instructions (2659 KB)

References

[1]. Zhang D, et al. α7 nicotinic receptor agonists reduce levodopa-induced dyskinesias with severe nigrostriatal damage. Mov Disord. 2015;30(14):1901-1911. [Content Brief]

[2]. Haig G, et al. The α7 Nicotinic Agonist ABT-126 in the Treatment of Cognitive Impairment Associated with Schizophrenia in Nonsmokers: Results from a Randomized Controlled Phase 2b Study. Neuropsychopharmacology. 2016;41(12):2893-2902. [Content Brief]

[3]. Gault LM, et al. ABT-126 monotherapy in mild-to-moderate Alzheimer's dementia: randomized double-blind, placebo and active controlled adaptive trial and open-label extension. Alzheimers Res Ther. 2016;8(1):44. Published 2016 Oct 18. [Content Brief]

Animal Administration
^[1]

Monkeys^[1]
MPTP-lesioned monkeys are used. All monkeys have been administered MPTP and exhibited mild to moderate parkinsonism. All monkeys are orally gavaged with L-dopa/carbidopa twice daily, which lead to the development of stable abnormal involuntary movements or dyskinesias. The treatment groups are as follows: vehicle-treated (n=6), nicotine-treated (n=5), Nelonicline treated (set 1, n=5) and Nelonicline-treated (set 2, n=5). These latter two sets of monkeys have previously been given ABT-894 and ABT-107 but using somewhat different treatment regimens. The present study is done after a 7 wk washout period, when LIDs are similar in all groups. Nelonicline is administered orally in a small cracker 30 min before L-dopa (10 mg/kg) and carbidopa (2.5 mg/kg). Nicotine, a positive control, is provided in the drinking water. Nelonicline is tested at 0.03, 0.10, 0.30 and 1.0 mg/kg, with each dose of Nelonicline tested for 1 or 2 wk^[1].

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

References

[1]. Zhang D, et al. α7 nicotinic receptor agonists reduce levodopa-induced dyskinesias with severe nigrostriatal damage. Mov Disord. 2015;30(14):1901-1911. [Content Brief]

[2]. Haig G, et al. The α7 Nicotinic Agonist ABT-126 in the Treatment of Cognitive Impairment Associated with Schizophrenia in Nonsmokers: Results from a Randomized Controlled Phase 2b Study. Neuropsychopharmacology. 2016;41(12):2893-2902. [Content Brief]

[3]. Gault LM, et al. ABT-126 monotherapy in mild-to-moderate Alzheimer's dementia: randomized double-blind, placebo and active controlled adaptive trial and open-label extension. Alzheimers Res Ther. 2016;8(1):44. Published 2016 Oct 18. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.1906 mL	15.9530 mL	31.9061 mL	79.7652 mL
	5 mM	0.6381 mL	3.1906 mL	6.3812 mL	15.9530 mL
	10 mM	0.3191 mL	1.5953 mL	3.1906 mL	7.9765 mL
	15 mM	0.2127 mL	1.0635 mL	2.1271 mL	5.3177 mL
	20 mM	0.1595 mL	0.7977 mL	1.5953 mL	3.9883 mL
	25 mM	0.1276 mL	0.6381 mL	1.2762 mL	3.1906 mL
	30 mM	0.1064 mL	0.5318 mL	1.0635 mL	2.6588 mL

Nelonicline Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Nelonicline1026134-63-3ABT-126ABT126ABT 126nAChRNicotinic acetylcholine receptorsselectiveoralschizophreniaAlzheimer'sdiseaseInhibitorinhibitorinhibit

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Nelonicline (Synonyms: ABT-126)

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