Galanthamine HBr

製品コードS1339 バッチS133902

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C17H21NO3.HBr

分子量 368.27 CAS No. 1953-04-4
Solubility (25°C)* 体外 Water 37 mg/mL (100.46 mM)
DMSO Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Galanthamineは、IC50 0.35 μMのAChE阻害剤であり、ブチリルコリンエステラーゼに対して50倍の選択性を示します。
in vitro Galanthamine has been demonstrated to have an IC50 of 14 nM and 15 nM on AChE in post-mortem human brain frontal cortex and the hippocampus region. Red-cell cholinesterase activity in blood samples from the neurosurgery patients is 10 times more strongly inhibited by Galanthamine in brain tissue samples. Galanthamine (1 μM) activates single channels with conductance's of 18 and 30 pS in outside-out patches excised from dexamethasone mouse fibroblasts (M10 cells). Galanthamine acts as noncompetitive nicotinic receptor agonists' on clonal rat pheochromocytoma (PC12) cells. Galanthamine (50 μM) activates single-channel currents in outside-out patches excised from clonal PC12 cells.
in vivo Galantamine significantly increases the number of living pyramidal neurons after ischemia-reperfusion injury. Galantamine significantly reduces TUNEL, active caspase-3, and SOD-2 immunoreactivity. The nicotinic antagonist mecamylamine blockes the protective effects of galantamine. The neuroprotective effects of galantamine are preserved even when first administered at 3 hours postischemia.

プロトコル(参考用のみ)

キナーゼアッセイ Acetylcholinesterase Assay
The catalytic activity of acetylcholinesterase in erythrocytes and brain is measured using [14C]acetylcholine iodide radiolabelled in the acetyl moiety at a final substrate concentration of 3.6 mmM, a pH of 7.4 and a temperature of 25 °C. Concentration response trials are then performed. After incubation of the sample with Galanthamine for 60 minutes at 25 °C in vitro, the catalytic reaction is started by the addition of substr
動物実験 動物モデル Gerbils
投薬量 10 mg/kg
投与方法 S.c. twice a day or 3 or 6 hours after ischemia and at subsequent 12-hours intervals until sacrifice

参考

  • https://pubmed.ncbi.nlm.nih.gov/1954303/
  • https://pubmed.ncbi.nlm.nih.gov/8071869/
  • https://pubmed.ncbi.nlm.nih.gov/7589215/
  • https://pubmed.ncbi.nlm.nih.gov/17526807/

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Antidementia medication acetylcholinesterase inhibitors have therapeutic benefits on osteoporotic bone by attenuating osteoclastogenesis and bone resorption [ J Cell Physiol, 2023, 10.1002/jcp.31057] PubMed: 37334837

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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