Galanthamine HBr

製品コードS1339 バッチS133903

化学情報

	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	10 mg/mL (27.15 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
キナーゼアッセイ	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/

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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

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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