Galanthamine HBr

製品コードS1339 バッチS133901

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 32 mg/mL (86.89 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 is an AChE inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase.
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. [1] 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). [2] 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. [3]
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. [4]

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

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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