Galanthamine HBr

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Galanthamine Hydrobromide 是一种长效、中枢活性乙酰胆碱酯酶 (AChE) 抑制剂 (IC50 = 410 nM) 和神经元烟碱 ACh 受体的变构增强剂。

Galanthamine hydrobromide is a long-acting, centrally active acetylcholinesterase(AChE) inhibitor (IC50 = 410 nM) and allosteric potentiator at neuronal nicotinic ACh receptors.(In Vitro):Galanthamine hydrobromide is 53-fold selectivity for AChE over butyrylcholinesterase.Galanthamine hydrobromide (25-1000 μM) inhibits both Aβ 1-40 (50 μM) and Aβ 1-42 (50 μM) aggregation.Galanthamine hydrobromide (25-1000 μM) protects against Aβ(1-40) and Aβ(1-42) toxicity in SH-SY5Y cells.Galanthamine hydrobromide also dramatically reduces Aβ(1-40)-induced cellular apoptosis.(In Vivo):Galanthamine hydrobromide (1.25-2.5 mg/kg; i.p. ) reduces cognitive deficits in APP23 mice.Galanthamine hydrobromide (10 mg/kg; i.g.) displays short elimination half-life of approximately 2 h in wild-type mice.

Galanthamine hydrobromide is 53-fold selectivity for AChE over butyrylcholinesterase.Galanthamine hydrobromide (25-1000 μM) inhibits both Aβ 1-40 (50 μM) and Aβ 1-42 (50 μM) aggregation.Galanthamine hydrobromide (25-1000 μM) protects against Aβ(1-40) and Aβ(1-42) toxicity in SH-SY5Y cells.Galanthamine hydrobromide also dramatically reduces Aβ(1-40)-induced cellular apoptosis.

Galanthamine hydrobromide (1.25-2.5 mg/kg; i.p. ) reduces cognitive deficits in APP23 mice.Galanthamine hydrobromide (10 mg/kg; i.g.) displays short elimination half-life of approximately 2 h in wild-type mice. Animal Model:APP23 mice Dosage:1.25 mg/kg, 2.5 mg/kg Administration:Intraperitoneal injection, daily, 1 week Result:Effectively remedied the spatial learning deficit.Animal Model:Female 57B1/6J wild type Dosage:10 mg/kg Administration:Oral gavage (Pharmacokinetic Analysis)Result:Cmax (0.31 μg/mL), t1/2β (1.6 h), AUC0-24h (0.67 μg ? h/mL).

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Endocrinology/Hormones

AChR

AChE

Neurological Disease

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1953-04-4

368.27

C17H21NO3·HBr

>98% (HPLC)

Water: 36 mg/mL (97.75 mM)

CN1CC[C@@]23C=C[C@@H](C[C@@H]2OC4=C(C=CC(=C34)C1)OC)O.Br

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(-20℃)

With Ice Pack

≥ 2 years