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

Anatabine dicitrate 

Cat. No.: HY-19918A
Handling Instructions

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.

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

Anatabine dicitrate Chemical Structure

Anatabine dicitrate Chemical Structure

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 299 In-stock
Estimated Time of Arrival: December 31
5 mg USD 250 In-stock
Estimated Time of Arrival: December 31
10 mg USD 350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1050 In-stock
Estimated Time of Arrival: December 31
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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].

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].

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

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 30 mg/mL (55.10 mM; Need ultrasonic)

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
10 mM 0.1837 mL 0.9183 mL 1.8367 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

Anatabine dicitrateNF-κBAmyloid-βnAChRNuclear factor-κBNuclear factor-kappaBβ-amyloid peptideAbetaNicotinic acetylcholine receptorsAlzheimer'sdiseaseanti-inflammatoryalkaloidAβ1-40Aβ1-42sAPPβBACE-1BBBα4β2Inhibitorinhibitorinhibit

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Anatabine dicitrate
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HY-19918A
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