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CAS NO.120786-18-7
98%(1-25)Kilogram98%(26-500)Kilogram98%(501-1000)Kilogram
| Molecular Formula | C15H18N2O |
| Molar Mass | 242.32 |
| Density | 1.20±0.1 g/cm3(Predicted) |
| Melting Point | 211-216oC |
| Boling Point | 505.0±50.0 °C(Predicted) |
| Specific Rotation(α) | D -147° (c = 0.36 in CH3OH) (Ayer); D24.5 -150.4° (c = 0.498 in MeOH) (Liu) |
| Solubility | Easily soluble in chloroform, soluble in methanol and ethanol, slightly soluble in water |
| Appearance | Crystallization (propanol) |
| Color | White to Almost white |
| pKa | 12.25±0.60(Predicted) |
| Storage Condition | Keep in dark place,Inert atmosphere,2-8°C |
| Refractive Index | 1.626 |
| MDL | MFCD01714949 |
| Physical and Chemical Properties | From the plant of the family of taxiaceae, Chian Tower, Huperzinaserrata(Thumb.), Trev |
| Use | Can effectively prevent the elderly brain neurasthenia, restore brain nerve function, activation of brain nerve transmission material |
| Melaleuca extract | Huperzine A is a natural plant alkali extracted from Melaleuca of the traditional Chinese medicine Huperzia. It is a powerful, reversible and highly selective second-generation acetylcholinesterase inhibitor. It has a slightly yellow to white crystalline powder in appearance, is easily soluble in chloroform, soluble in methanol and ethanol, slightly soluble in water, has high fat solubility, small molecules, it can penetrate the blood-brain barrier well. After entering the center, it is more distributed in the frontal lobe, temporal lobe, hippocampus and other brain areas that are closely related to learning and memory. It has a strong inhibitory effect on acetylcholinesterase (AchE) at a low dose, which significantly increases the content of acetylcholine (Ach) in the synaptic gap in the distribution area, thereby enhancing the excitation of neurons, strong chemistry The exciting effect of learning and memory brain areas can improve cognitive function, enhance memory retention and promote memory reproduction. It is currently the most successful drug developed in China to treat Alzheimer's disease (Alzheimer's disease). |
| acetylcholinesterase | acetylcholinesterase is an enzyme that decomposes the neurotransmitter acetylcholine in the brain, responsible for a large number of neuronal synaptic functions and central nervous system nerve excitement. One acetylcholinesterase molecule can reduce the function of about 25,000 B acylcholine molecules. Inhibitors of this enzyme are often used to make nerve gas preparations, because too much acetylcholine in the body can cause muscle paralysis and asphyxia. people with Alzheimer's disease often lack acetylcholine because acetylcholine plays an important role in nerve stimulation, memory and learning, and excitement. Reducing acetylcholinesterase levels can release acetylcholine and allow more neurons to move. |
| indications | huperzine a is a reversible potent cholinesterase inhibitor, which is stronger than physostigmine, neostigmine and Tacrine. For myasthenia gravis, the effective rate is 99%. Clinical trials have shown that this product is suitable for benign memory disorders, and can improve patients' abilities such as pointing memory, associative learning, image recall, meaningless graphic recognition, and portrait recall. It also enhances the learning and memory of normal people; This product can also improve memory disorders caused by dementia patients and organic brain diseases. Huperzine A can be applied to the treatment of the following symptoms: 1, used to treat and improve the memory function of middle-aged and elderly people, and to improve the function of associative recall; used for memory loss caused by excessive brain use, Improve learning and work efficiency; 2, used for neurasthenia with memory dysfunction; 3, Huperzine A is used for memory loss caused by cerebrovascular disorders; 4, it is used to improve the memory of senile dementia, and it has obvious effect on improving and restoring the cognition and memory function of patients and improving emotional and behavioral abnormalities; 5, it is used to treat myasthenia gravis; 6, Huperzine A can improve the association disorder, cognitive function, memory loss, etc. associated with schizophrenia; 7, it can improve memory function accompanied by various brain diseases and somatic diseases |
| side effects | skin urticaria, abdominal pain, salivation, muscle twitching, diarrhea and insomnia, but not common. Excessive dose can cause dizziness, nausea, gastrointestinal discomfort, chest tightness, fatigue, bradycardia and other reactions. Generally, it can disappear by itself. When the reaction is obvious, it can be relieved and disappeared after the dose is reduced or the drug is stopped. |
| Inhibitory effect | Huperzine A has a selective inhibitory effect on true cholinesterase, and the inhibitory intensity is thousands of times that of false cholinesterase; the inhibition method is competitive and non-competitive mixed inhibition, which is significantly different from pure competitive inhibitors ; it is easy to enter the center through the blood-brain barrier, and has both central and peripheral therapeutic effects; the effective time is long; good absorption from gastrointestinal tract; High safety index; Good stability. the comparative results of the inhibitory intensity of different drugs on acetylcholinesterase (AChE) are: huperzine a> physostigmine> neostigmine> huperzine B> galantamine> galantamine. the inhibition intensity of human butyrylcholinesterase (BuChE) is as follows: physostigmine> neostigmine> huperzine a> huperzine B. The effect of this product on strengthening the amplitude of muscle contraction caused by indirect electrical stimulation of nerves and enhancing the memory function of rats are stronger than physostigmine, but the toxicity is lower than physostigmine, and the action time is long. |
| determination of huperzine a content by HPLC | [test article] Huperzia serrata (Thunb) Trev, a Huperaceae plant. The extract is processed into a capsule. (1) chromatographic conditions: chromatographic column: Alltima C18 column (4.6mm × 150mm), mobile phase: methanol -0.1mol/L ammonium acetate buffer (pH6.0) (36:64); Flow rate: 0.6 ml/min; Detection wavelength: 308nm; Column temperature: room temperature. (2) preparation of reference substance solution: take appropriate amount of huperzine a reference substance and add mobile phase to prepare a reference substance solution containing 0.005mg per milliliter. (3) preparation of sample solution: take appropriate amount of huperzine a capsule (equivalent to huperzine a 0.125mg), place it in a 25ml volumetric flask, dissolve it with mobile phase and dilute it to scale, shake well, and serve as sample solution. (4) determination: 20 μl of reference substance and 20 μl of sample solution respectively were taken for sample analysis. |
| use | can effectively prevent brain neurasthenia in middle-aged and elderly people, restore brain nerve function and activate brain nerve transmission substances. it is currently a new drug for the treatment of benign memory impairment. Reversible alkaloid inhibitor of AChE which crosses the blood-brain barrier. A potential therapeutic agent for Alzheimer holmium disease. It reduces cell death induced by glutamate in primary cultures der ived from forebrain, hippocampus, cortex and cerebellum of embryonic rat brain. huperzine a not only inhibits cholinesterase activity, but also affects free radical system, reduce the content of somatostatin, intracellular [Ca2 +] and glutamic acid, increase the expression level of calmodulin (CaM) and calmodulin messenger ribonucleic acid (CaM mRNA) and other pharmacological mechanisms, and improve cognitive function and learning and memory ability. |
CAS:
120786-18-7
MF:
C15H18N2O
MW:
242.32
EINECS:
200-001-8
MDL No.:
MFCD00171439
Boiling point:
505.0±50.0 °C(Predicted)
Density
1.20±0.1 g/cm3(Predicted)
storage temp.
2-8°C
solubility
DMSO : ≥ 50 mg/mL (206.34 mM)
form
solid
pka
12.25±0.60(Predicted)
color
White or off-white
InChI
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+
InChIKey
ZRJBHWIHUMBLCN-QDEBKDIKSA-N
SMILES
C12CC3/C(=C\C)/C(N)(C=1C=CC(=O)N2)CC(C)=C3
Xi'an Eastling biotech Co., Ltd. is dedicated to the research and development, production, and sales of natural plant extracts; With nearly 15 years of experience in identifying, researching, developing, and producing active ingredients for medicinal plants, we focus on providing innovative products and services to customers in industries such as pharmaceuticals, health food, and cosmetics.
Eastling Biotechnology has established a global direct harvesting system for plant raw materials, ensuring the high quality and authenticity of raw materials, while also protecting the continuity and diversity of plants; Having strong research and development capabilities, we can develop more effective and specialized plant active ingredients for the pharmaceutical, health food, and cosmetics industries; We have established an advanced quality control system, and the quality control of our products depends on advanced testing instruments and high-level technical experts. The effective combination of the two forms Eastling's ability to quickly and rigorously control product quality.
We have a production system that complies with Chinese GMP and American cGMP certifications, as well as advanced and optimized large-scale industrial production technology. In addition to producing specific products for Eastling Biotechnology, we also provide customized services to meet the characteristics and needs of different customers to produce customized products.
We believe that natural active ingredients are the foundation of our service to customers. Scientific and effective production technology is the foundation for us to provide customers with specialized products. We have the ability to serve customers in the pharmaceutical, health food, and cosmetics industries, provide new product solutions, and add new value to their products.