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| 10mg |
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Purity: ≥98%
(-)-Huperzine A (Hup A; Selagine; (-)-Selagine) is a naturally occurring, highly specific and reversible inhibitor of acetylcholinesterase (AChE) with neuroprotective activity. It inhibits AChE with Ki of 7 nM, and exhibits 200-fold more selectivity for G4 AChE over G1 AChE. Chemically, (-)-Huperzine A is an active Lycopodium alkaloid isolated from traditional Chinese herb. It also acts as an NMDA receptor antagonist. (-)-Huperzine A has been investigated as a possible treatment for diseases characterized by neurodegeneration-particularly Alzheimer's disease. Huperzine A is also marketed as a dietary supplement with claims made for its ability to improve memory and mental function.
| ln Vitro |
(-)-Huperzine A (1 μM; 2 hours) attenuates neuronal damage caused by Aβ23-35 (20 μM) [2]. (-)-Huperzine A (100 μM) reversibly suppresses NMDA-induced currents (IC50=126 μM) in whole-cell voltage-clamp recordings in CA1 pyramidal neurons that had been acutely separated from the rat hippocampal [3].
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| ln Vivo |
In rats with degeneration brought on by icv infusion of beta-amyloid-(1-40), (-)-Huperzine A (0.1-0.2 mg/kg; intraperitoneal injection; daily; for 12 days) lessens neuronal damage and cognitive dysfunction [5].
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| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats (220-280 g)[5]
Doses: 0.1 mg/kg, 0.2 mg/kg Route of Administration: intraperitoneal (ip)injection, daily, for 12 days Experimental Results: Partly reversed the down-regulation of anti-apoptotic Bcl-2 and the up-regulation of pro-apoptotic Bax and P53 proteins and decreased the apoptosis that normally followed b-amyloid injection; alleviated the cognitive dysfunction induced by b-amyloid protein-(1-40). |
| References |
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| Additional Infomation |
Huperzine A is a sesquiterpene alkaloid isolated from a club moss Huperzia serrata that has been shown to exhibit neuroprotective activity. It is also an effective inhibitor of acetylcholinesterase and has attracted interest as a therapeutic candidate for Alzheimer's disease. It has a role as an EC 3.1.1.7 (acetylcholinesterase) inhibitor, a neuroprotective agent, a plant metabolite and a nootropic agent. It is a sesquiterpene alkaloid, a pyridone, a primary amino compound and an organic heterotricyclic compound. It is a conjugate base of a huperzine A(1+).
Huperzine A, is a naturally occurring sesquiterpene alkaloid found in the extracts of the firmoss Huperzia serrata. The botanical has been used in China for centuries for the treatment of swelling, fever and blood disorders. Recently in clinical trials in China, it has demonstrated neuroprotective effects. It is currently being investigated as a possible treatment for diseases characterized by neurodegeneration – particularly Alzheimer’s disease. Huperzine A has been reported in Aspergillus versicolor, Phlegmariurus phlegmaria, and other organisms with data available. Drug Indication Investigated for use/treatment in alzheimer's disease. Mechanism of Action Huperzine A has been found to be an inhibitor of the enzyme acetylcholinesterase. This is the same mechanism of action of pharmaceutical drugs such as [galantamine] and [donepezil] used to treat Alzheimer's disease. Pharmacodynamics Huperzine A is an alkaloid derived from Huperzia serrata (which is available as an herbal product in the US). It is under investigation as an acetylcholinesterase inhibitor. Clinical trials in China have shown that huperzine A is comparably effective to the drugs currently on the market, and may even be somewhat safer in terms of side effects. |
| Molecular Formula |
C15H18N2O
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| Molecular Weight |
242.32
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| Exact Mass |
242.141
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| CAS # |
102518-79-6
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| Related CAS # |
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| PubChem CID |
854026
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
479.5±25.0 °C at 760 mmHg
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| Melting Point |
211-216oC
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| Flash Point |
243.8±23.2 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.741
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| LogP |
-0.22
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
18
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| Complexity |
551
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C/C=C/1\[C@@H]2CC3=C([C@]1(CC(=C2)C)N)C=CC(=O)N3
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| InChi Key |
ZRJBHWIHUMBLCN-YQEJDHNASA-N
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| InChi Code |
InChI=1S/C15H18N2O/c1-3-11-10-6-9(2)8-15(11,16)12-4-5-14(18)17-13(12)7-10/h3-6,10H,7-8,16H2,1-2H3,(H,17,18)/b11-3+/t10-,15+/m0/s1
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| Chemical Name |
(1R,9R,13E)-1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.02,7]trideca-2(7),3,10-trien-5-one
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.32 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.32 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% propylene glycol, 5% Tween 80, 65% D5W:30 mg/mL |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01676311 | Terminated Has Results | Drug: Huperzine A Drug: Placebo |
Traumatic Brain Injury | Spaulding Rehabilitation Hospital | December 2013 | Phase 2 |
| NCT01194336 | Completed | Drug: Huperzine A Drug: Donepezil Drug: Galantamine Other: Placebo |
Biomarkers, Pharmacological | U.S. Army Medical Research and Development Command |
February 2012 | |
| NCT05518578 | Recruiting | Drug: SPN-817 | Epilepsy Seizures, Epileptic |
Supernus Pharmaceuticals, Inc. | February 7, 2023 | Phase 2 |
| NCT01136551 | Unknown † | Drug: Huperzine A | Healthy Bioavailability |
Hadassah Medical Organization | September 2010 | Not Applicable |
| NCT01282619 | Unknown † | Drug: Huperzine A Drug: huperzine A Drug: Placebo |
Alzheimer's Disease | Shandong Luye Pharmaceutical Co., Ltd. | May 2010 | Phase 2 Phase 3 |
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