1. NF-κB Membrane Transporter/Ion Channel Neuronal Signaling
  2. NF-κB Amyloid-β nAChR
  3. Anatabine dicitrate

Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potent α4β2 nAChR agonist. Anatabine dicitrate inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.

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Anatabine dicitrate Chemical Structure

Anatabine dicitrate Chemical Structure

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 299 In-stock
Solution
10 mM * 1 mL in DMSO USD 299 In-stock
Solid
5 mg USD 250 In-stock
10 mg USD 350 In-stock
50 mg USD 650 In-stock
100 mg USD 1050 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potent α4β2 nAChR agonist. Anatabine dicitrate inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment[1][2][3].

IC50 & Target

NF-κB[1]
Amyloid-β (Aβ)[1]
α4β2 nAChR[2]

In Vitro

Anatabine (600 μg/mL; 24 hours; SHSY-5Y cells) treatment shows an inhibition of p65 NF-κB phosphorylation[1].
Anatabine (500-1000μg/mL; 30 minutes; SHSY-5Y cells) treatment fully prevents the increase in BACE-1 mRNA levels induced by TNF-α. After 24 hours, Anatabine treatment shows a dose-dependent inhibition of BACE-1 protein levels[1].
Anatabine dose dependently inhibits Aβ1-40 and Aβ1-42 with an approximate half maximal inhibitory concentration of 640 μg/mL for both Aβ1-40 and Aβ1-42 in 7W CHO cells. Anatabine inhibits sAPPβ secretion without impacting sAPPα suggesting that Anatabine is preventing the β-cleavage of amyloid precursor protein (APP)[1].

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

Western Blot Analysis[1]

Cell Line: SHSY-5Y cells
Concentration: 600 μg/mL
Incubation Time: 24 hours
Result: An inhibition of p65 NF-κB phosphorylation was observed.

RT-PCR[1]

Cell Line: SHSY-5Y cells
Concentration: 500 μg/mL, 1000 μg/mL
Incubation Time: 30 minutes
Result: Fully prevented the increase in BACE-1 mRNA levels induced by TNF-α.
In Vivo

Anatabine (0.5-2 mg/kg; intraperitoneal injection; daily; for 4 days; transgenic mouse) treatment significantly lowers brain soluble Aβ1-40 and Aβ1-42 levels in a transgenic mouse model of Alzheimer's disease[1].

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

Animal Model: Transgenic mice overexpressing the human APP695sw mutation and the presenilin-1 mutation M146L (Tg PS1/APPsw) (50 week-old)[1]
Dosage: 0.5 mg/kg, 2 mg/kg
Administration: Intraperitoneal injection; daily; for 4 days
Result: Significantly lowered brain soluble Aβ1-40 and Aβ1-42 levels in a transgenic mouse model of Alzheimer's disease.
Molecular Weight

544.46

Formula

C22H28N2O14

Appearance

Solid

Color

White to off-white

SMILES

O=C(CC(C(O)=O)(O)CC(O)=O)O.O=C(CC(C(O)=O)(O)CC(O)=O)O.[C@@H]1(C2=CC=CN=C2)CC=CCN1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (183.67 mM; Need ultrasonic)

DMSO : 30 mg/mL (55.10 mM; Need ultrasonic; 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 1.8367 mL 9.1834 mL 18.3668 mL
5 mM 0.3673 mL 1.8367 mL 3.6734 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 (sealed storage, 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 50 mg/mL (91.83 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.03%

References

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 (sealed storage, 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 1.8367 mL 9.1834 mL 18.3668 mL 45.9171 mL
5 mM 0.3673 mL 1.8367 mL 3.6734 mL 9.1834 mL
10 mM 0.1837 mL 0.9183 mL 1.8367 mL 4.5917 mL
15 mM 0.1224 mL 0.6122 mL 1.2245 mL 3.0611 mL
20 mM 0.0918 mL 0.4592 mL 0.9183 mL 2.2959 mL
25 mM 0.0735 mL 0.3673 mL 0.7347 mL 1.8367 mL
30 mM 0.0612 mL 0.3061 mL 0.6122 mL 1.5306 mL
40 mM 0.0459 mL 0.2296 mL 0.4592 mL 1.1479 mL
50 mM 0.0367 mL 0.1837 mL 0.3673 mL 0.9183 mL
H2O 60 mM 0.0306 mL 0.1531 mL 0.3061 mL 0.7653 mL
80 mM 0.0230 mL 0.1148 mL 0.2296 mL 0.5740 mL
100 mM 0.0184 mL 0.0918 mL 0.1837 mL 0.4592 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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.

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Anatabine dicitrate
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