1. Neuronal Signaling
    Apoptosis
    Membrane Transporter/Ion Channel
  2. AChE
    Apoptosis
    iGluR
  3. (-)-Huperzine A

(-)-Huperzine A (Synonyms: Huperzine A)

Cat. No.: HY-17387 Purity: >98.0%
Handling Instructions

(-)-Huperzine A (Huperzine A) is an alkaloid isolated from a Chinese club moss, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease.

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

(-)-Huperzine A Chemical Structure

(-)-Huperzine A Chemical Structure

CAS No. : 102518-79-6

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Description

(-)-Huperzine A (Huperzine A) is an alkaloid isolated from a Chinese club moss, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease[1][2][3][4][5].

IC50 & Target

IC50: 82 nM (AChE) [1], NMDA[3]

In Vitro

(-)-Huperzine A (1 µM; 2 hours) attenuates Aβ23-35 (20 µM)-induced neuronal injury[2].
(-)-Huperzine A (100μM) reversibly inhibits the NMDA-induced current (IC50=126 μM) in whole-cell voltage-clamp recording in CA1 pyramidal neurons acutely dissociated from rat hippocampus[3].

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

In Vivo

(-)-Huperzine A (0.1-0.2 mg/kg; i.p.; daily; for 12 days) can alleviate the cognitive dysfunction and neuronal degeneration induced by i.c.v. infusion of beta-amyloid protein-(1-40) in rats[5].

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

Animal Model: Male Sprague-Dawley rats (220-280 g)[5]
Dosage: 0.1 mg/kg, 0.2 mg/kg
Administration: Intraperitoneal injection, daily, for 12 days
Result: Partly reversed the down-regulation of anti-apoptotic Bcl-2 and the up-regulation of pro-apoptotic Bax and P53 proteins and reduced the apoptosis that normally followed b-amyloid injection; alleviated the cognitive dysfunction induced by b-amyloid protein-(1–40).
Clinical Trial
Molecular Weight

242.32

Formula

C₁₅H₁₈N₂O

CAS No.

102518-79-6

SMILES

O=C1NC2=C([[email protected]@](/C3=C\C)(N)CC(C)=C[[email protected]@]3([H])C2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (412.68 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.1268 mL 20.6339 mL 41.2677 mL
5 mM 0.8254 mL 4.1268 mL 8.2535 mL
10 mM 0.4127 mL 2.0634 mL 4.1268 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: ≥ 2.5 mg/mL (10.32 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (10.32 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (10.32 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

(-)-Huperzine AHuperzine AAChEApoptosisiGluRAcetylcholinesteraseIonotropic glutamate receptorsneuroprotectiveneurodegenerativediseasesAlzheimer'sdiseasecognitive-enhancingcholinergicnon-cholinergiceffectsneuropathicpainanti-cholinesteraseInhibitorinhibitorinhibit

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(-)-Huperzine A
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