Nelonicline (Synonyms: ABT-126)

Name: Nelonicline
Brand: MedChemExpress
SKU: HY-16748
Rating: 4.5 (0 reviews)

製品番号: HY-16748 純度: 99.82%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Nelonicline 構造式

CAS 番号 : 1026134-63-3

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 841	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 841	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$320	在庫あり	Estimated Time of Arrival: December 31
5 mg	$765	在庫あり	Estimated Time of Arrival: December 31
10 mg	$1220	在庫あり	Estimated Time of Arrival: December 31
25 mg	$2210	在庫あり	Estimated Time of Arrival: December 31
50 mg	$3320	在庫あり	Estimated Time of Arrival: December 31
100 mg	$4980	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 0 publication(s) in Google Scholar

Other Forms of Nelonicline:

Nelonicline citrate お問い合わせ

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

生物活性
プロトコル
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target

Neuronal nicotinic receptor^[1]

体外実験

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.

分子量

313.42

分子式

C₁₇H₁₉N₃OS

CAS 番号

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, stored under nitrogen, away from moisture

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

溶剤 & 溶解度

体外:

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)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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.

純度とドキュメンテーション

純度: 99.82%

Select Batch:

データシート (276 KB) SDS (252 KB)

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

取扱説明書 (2659 KB)

参考文献

[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]

動物実験
^[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。

参考文献

[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

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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

最近チェックした製品:

製品名

カスタマ需要量 *

お名前 *

タイトル

メールアドレス *

電話番号 *

デパートメント

組纖名 *

市区町村

都道府県

国或いは地域 *

必ず会社名を記載ください。個人への返信は行いません。

備考

製品名

Lot #

お名前 *

メールアドレス *

電話番号 *

部門 *

組纖名 *

国或いは地域 *

備考

お名前
メール *

	Sorry, but the email address you supplied was invalid.

Nelonicline (Synonyms: ABT-126)

カスタマーレビュー

Other Forms of Nelonicline:

Nelonicline 関連抗体

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

Nelonicline 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Nelonicline Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

カスタマーレビュー

Request for HNMR Report

Request for HNMR Report