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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Galanthamine HBr (Razadyne, Reminyl), the hydrobromide salt of Galanthamine, is a centrally active and long-acting AChE/acetylcholinesterase inhibitor approved for the treatment of cognitive decline in Alzheimer's disease and various other memory impairments. It inhibits AChE with an IC50 of 0.35 μM, and shows > 50-fold selectivity over butyryl-cholinesterase.
| ln Vitro |
AChE has a 53-fold selectivity for galanthamine hydrobromide compared to butyrylcholinesterase[2]. Aβ 1-40 (50 µM) and Aβ 1-42 (50 µM) aggregation are both inhibited by galanthamine hydrobromide (25-1000 µM)[4]. In SH-SY5Y cells, galantamine hydrobromide (25–1000 µM) guards against Aβ(1-42) and Aβ(1–40) toxicity[4]. Moreover, galanthamine hydrobromide significantly lessens cellular apoptosis brought on by Aβ(1–40)[4].
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| ln Vivo |
In APP23 mice, galanthamine hydrobromide (1.25–2.5 mg/kg; ip) lessens cognitive deficits[5]. In wild-type mice, galantamine hydrobromide (10 mg/kg; ig) exhibits a brief elimination half-life of roughly two hours[6].
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| Animal Protocol |
Animal/Disease Models: APP23 mice[5]
Doses: 1.25 mg/kg, 2.5 mg/kg Route of Administration: intraperitoneal (ip)injection, daily, 1 week Experimental Results: Effectively remedied the spatial learning deficit. Animal/Disease Models: Female 57B1/6J wild type[6] Doses: 10 mg/kg Route of Administration: po (oral gavage) (pharmacokinetic/PK Analysis) Experimental Results: Cmax (0.31 µg/mL), t1/2β (1.6 h), AUC0-24h (0.67 µg • h/mL). |
| References | |
| Additional Infomation |
Galantamine Hydrobromide is the hydrobromide salt form of galantamine, a tertiary alkaloid obtained synthetically or naturally from the bulbs and flowers of Narcissus and several other genera of the Amaryllidaceae family with anticholinesterase and neurocognitive-enhancing activities. Galantamine competitively and reversibly inhibits acetylcholinesterase, thereby increasing the concentration and enhancing the action of acetylcholine (Ach). In addition, galantamine is a ligand for nicotinic acetylcholine receptors, which may increase the presynaptic release of Ach and activate postsynaptic receptors. This agent may improve neurocognitive function in mild and moderate Alzheimer' s disease and may reduce abstinence-induced cognitive symptoms that promote smoking relapse.
A benzazepine derived from norbelladine. It is found in GALANTHUS and other AMARYLLIDACEAE. It is a cholinesterase inhibitor that has been used to reverse the muscular effects of GALLAMINE TRIETHIODIDE and TUBOCURARINE and has been studied as a treatment for ALZHEIMER DISEASE and other central nervous system disorders. See also: Galantamine (has active moiety). |
| Molecular Formula |
C17H21NO3.HBR
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|---|---|---|
| Molecular Weight |
368.27
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| Exact Mass |
367.078
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| CAS # |
1953-04-4
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| Related CAS # |
Galanthamine;357-70-0;Galanthamine-d3 hydrobromide
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| PubChem CID |
121587
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| Appearance |
White to off-white solid powder
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| Melting Point |
256 °C
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
-95 ° (C=1.4, H2O)
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| LogP |
2.746
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
22
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| Complexity |
440
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CN1CC[C@@]23C=C[C@@H](C[C@@H]2OC4=C(C=CC(=C34)C1)OC)O.Br
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| InChi Key |
QORVDGQLPPAFRS-XPSHAMGMSA-N
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| InChi Code |
InChI=1S/C17H21NO3.BrH/c1-18-8-7-17-6-5-12(19)9-14(17)21-16-13(20-2)4-3-11(10-18)15(16)17;/h3-6,12,14,19H,7-10H2,1-2H3;1H/t12-,14-,17-;/m0./s1
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| Chemical Name |
(1S,12S,14R)-9-methoxy-4-methyl-11-oxa-4-azatetracyclo[8.6.1.01,12.06,17]heptadeca-6(17),7,9,15-tetraen-14-ol;hydrobromide
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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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: ≥ 1.25 mg/mL (3.39 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 12.5 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: ≥ 1.25 mg/mL (3.39 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 12.5 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: ≥ 1.25 mg/mL (3.39 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: Saline: 20 mg/mL Solubility in Formulation 5: 10 mg/mL (27.15 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7154 mL | 13.5770 mL | 27.1540 mL | |
| 5 mM | 0.5431 mL | 2.7154 mL | 5.4308 mL | |
| 10 mM | 0.2715 mL | 1.3577 mL | 2.7154 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.
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