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Galanthamine HBr/氢溴酸加兰他敏 {[allProObj[0].p_purity_real_show]}

货号:A523680 同义名: Galantamine hydrobromide; Galanthamine hydrobromide

Galanthamine HBr 是一种天然 AchE 抑制剂(IC50 410 nM),作为神经元 nAchRs 的变构增强剂,常用于轻度至中度阿尔茨海默病及记忆障碍的研究。

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Galanthamine HBr/氢溴酸加兰他敏 化学结构 CAS号:1953-04-4
Galanthamine HBr/氢溴酸加兰他敏 化学结构
CAS号:1953-04-4
Galanthamine HBr/氢溴酸加兰他敏 3D分子结构
CAS号:1953-04-4
Galanthamine HBr/氢溴酸加兰他敏 化学结构 CAS号:1953-04-4
Galanthamine HBr/氢溴酸加兰他敏 3D分子结构 CAS号:1953-04-4
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Galanthamine HBr/氢溴酸加兰他敏 纯度/质量文件 产品仅供科研

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Galanthamine HBr/氢溴酸加兰他敏 生物活性

靶点
  • AChE

    AChE, IC50:0.35 μM

描述 Galanthamine Hydrobromide is acetylcholinesterase inhibitor (AChEI) and a neuroactive drug capable of passing through the blood–brain barrier and can slow down the effects of AD[3]. Incubation of the cells for 48 h with 300 nM galantamine doubled the density of α7 nicotinic receptors and tripled the expression of the antiapoptotic protein Bcl-2[4]. Moreover, pretreatment with galantamine (8 mg/kg, i.m.) prevented the reduction of EPSC (excitatory postsynaptic currents) frequency observed at 6-9 days after the soman challenge[5].

Galanthamine HBr/氢溴酸加兰他敏 细胞实验

Cell Line
Concentration Treated Time Description References
HT-22 cells 10 μM 24 hours To investigate the effect of galantamine on Mi-sup-induced inflammatory response in HT-22 cells. Galantamine reduced the Mi-sup-induced increase in NF-κB p65 levels and expression of pro-inflammatory cytokines (IL-1β and IL-6). J Neuroinflammation. 2018 Apr 18;15(1):112
BV-2 cells 10 μM 24 hours To investigate the effect of galantamine on LPS-induced inflammatory response in BV-2 cells. Galantamine reduced the LPS-induced increase in NF-κB p65 levels. J Neuroinflammation. 2018 Apr 18;15(1):112
α7 nACh receptors stably expressed in HEK293 cells 10 nM to 10 μM 40 s pre-application (60 s for 0.01 μM), followed by 250 ms co-application with ACh To validate modulatory effects of galanthamine on α7 nACh receptors in HEK293 cells. Results aligned with oocyte experiments, showing no positive modulation and inhibition at high concentrations (100 μM). Br J Pharmacol. 2018 Jul;175(14):2911-2925
RAW 264.7 cells 10 μmol/L 24 hours To investigate the effect of Galanthamine on LPS-induced migration of RAW 264.7 cells, results showed that Galanthamine significantly inhibited LPS-induced cell migration. Acta Pharm Sin B. 2020 Oct;10(10):1926-1942

Galanthamine HBr/氢溴酸加兰他敏 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Kunming mice LPS-induced neuroinflammation model Intraperitoneal injection 4 mg/kg Once daily for 14 days To investigate the effect of galantamine on LPS-induced cognitive impairment and neuroinflammation. Galantamine improved LPS-induced deficits in spatial learning and memory, reduced the expression of CD11b, GFAP, NF-κB p65, and pro-inflammatory cytokines in the hippocampus, and increased the levels of synapse-associated proteins (SYN and PSD-95). J Neuroinflammation. 2018 Apr 18;15(1):112
Wistar rats Adolescent intermittent ethanol (AIE) exposure model Intraperitoneal injection 4 mg/kg In the prevention study, administered 30 min prior to each gavage, totaling 16 doses; in the restoration study, administered daily for 2 weeks starting from P57 Galanthamine prevented and reversed AIE-induced neuroimmune signaling and loss of hippocampal neurogenesis. In the prevention study, galantamine pretreatment blocked AIE induction of CCL2, HMGB1, and COX-2, and prevented the reduction in neurogenesis. In the restoration study, galantamine treatment reversed AIE induction of these inflammatory markers and restored neurogenesis. J Neuroinflammation. 2021 Sep 16;18(1):212
Mice Caerulein-induced acute pancreatitis model Intraperitoneal injection 1, 4, or 6 mg/kg body weight Administered once 1 hour before the first caerulein injection and again 30 minutes after the third injection Galanthamine significantly attenuated pancreatic histologic injury, reflected by a reduction in serum amylase and pancreatic inflammatory cytokines and an increase in the anti-inflammatory cytokine IL-10 in the serum. These beneficial effects were not altered by bilateral subdiaphragmatic vagotomy, knockout of either choline acetyltransferase-positive T cells or α7nAChR, or administration of the nAChR ganglionic blocker mecamylamine or the more selective α7nAChR antagonist methyllycaconitine. Mol Med. 2023 Oct 31;29(1):149
Mice Opa1–/– mice and aged WT mice Oral 3.28 mg/kg bodyweight/d Daily for 90 days (Opa1–/– mice) or 18 weeks (aged mice) RJx-01 (containing Galanthamine) improved muscle function, reduced denervation, decreased inflammatory markers, ameliorated mitochondrial morphology and autophagy, and increased satellite cell content. JCI Insight. 2023 Aug 8;8(15):e168787
Mice FMF-KI mice (MefvV726A/V726A) Intraperitoneal injection 4-12 mg/kg (escalated by 4 mg every 2 weeks) Twice daily for 8 weeks To assess the impact of long-term Galanthamine on chronic inflammation in FMF-KI mice. Results demonstrated significant attenuation of splenomegaly, reduced inflammatory cell infiltration (e.g., spleen and subcutaneous air pouch), decreased serum amyloid A (SAA) levels, and improved anemia. Notably, Galanthamine's effects persisted in vagotomized or α7nAChR-KO mice, suggesting a mechanism independent of the classical cholinergic anti-inflammatory pathway. Mol Med. 2022 Dec 9;28(1):148
Sprague-Dawley rats Cardiac ischemia/reperfusion (I/R) model Isolated heart perfusion 5 × 10^-8 M 30 min ischemia followed by 40 min reperfusion To investigate the effect of galantamine on cardiac ischemia/reperfusion injury in isolated hearts. Results showed that galantamine treatment significantly improved left ventricular function (LVDP, ±dP/dt, WP) without affecting heart rate. Mol Med. 2017 Jul;23:120-133
Male adult Wistar rats Experimental model of dementia induced by scopolamine Intraperitoneal injection 1 mg/kg For 9 consecutive days To evaluate the neuroprotective effects of galantamine in scopolamine-induced dementia in rats. Results showed that galantamine significantly increased brain ACh levels, improved recognition memory and habituation, and restored the cholinergic system influence index. Antioxidants (Basel). 2022 Feb 12;11(2):374
NOD mice Type 1 diabetes model Intraperitoneal injection 1 mg/kg Daily for 20 weeks To study the preventive effects of galantamine in type 1 diabetes, results showed that galantamine significantly delayed the onset of hyperglycemia, reduced pancreatic islet inflammation, and decreased serum levels of anti-insulin antibodies. Mol Med. 2015 Nov;21(1):702-708

Galanthamine HBr/氢溴酸加兰他敏 参考文献

[1]Pereira EF, Alkondon M, et al. Physostigmine and galanthamine: probes for a novel binding site on the alpha 4 beta 2 subtype of neuronal nicotinic acetylcholine receptors stably expressed in fibroblast cells. J Pharmacol Exp Ther. 1994 Aug;270(2):768-78.

[2]Thomsen T, Kaden B, et al. Inhibition of acetylcholinesterase activity in human brain tissue and erythrocytes by galanthamine, physostigmine and tacrine. Eur J Clin Chem Clin Biochem. 1991 Aug;29(8):487-92.

[3]Woo FY, Basri M, Masoumi HR, Ahmad MB, Ismail M. Formulation optimization of galantamine hydrobromide loaded gel drug reservoirs in transdermal patch for Alzheimer's disease. Int J Nanomedicine. 2015 Jun 5;10:3879-86.

[4]Arias E, Alés E, Gabilan NH, Cano-Abad MF, Villarroya M, García AG, López MG. Galantamine prevents apoptosis induced by beta-amyloid and thapsigargin: involvement of nicotinic acetylcholine receptors. Neuropharmacology. 2004 Jan;46(1):103-14.

[5]Alexandrova EA, Alkondon M, Aracava Y, Pereira EF, Albuquerque EX. Galantamine prevents long-lasting suppression of excitatory synaptic transmission in CA1 pyramidal neurons of soman-challenged guinea pigs. Neurotoxicology. 2014 Sep;44:270-8.

Galanthamine HBr/氢溴酸加兰他敏 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.72mL

0.54mL

0.27mL

13.58mL

2.72mL

1.36mL

27.15mL

5.43mL

2.72mL

Galanthamine HBr/氢溴酸加兰他敏 技术信息

CAS号1953-04-4
分子式C17H22BrNO3
分子量 368.27
SMILES Code O[C@H]1C=C[C@@]23CCN(C)CC4=CC=C(OC)C(O[C@@]3([H])C1)=C24.Br
MDL No. MFCD00067672
别名 Galantamine hydrobromide; Galanthamine hydrobromide; NSC 100058; Galanthamine; Galantamine (hydrobromide)
运输蓝冰
InChI Key QORVDGQLPPAFRS-XPSHAMGMSA-N
Pubchem ID 121587
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, store in freezer, under -20°C

溶解方案

DMSO: 12 mg/mL(32.59 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 15 mg/mL(40.73 mM),配合低频超声,并水浴加热至45℃助溶

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
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