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加兰他敏, 乙酰胆碱酯酶抑制剂(卡特赖特血型)

有效的选择性\ xa0乙酰胆碱酯酶抑制剂。
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货号 (SKU) 包装规格 是否现货 价格 数量
G125955-20mg
20mg 现货 Stock Image
G125955-100mg
100mg 现货 Stock Image
G125955-500mg
500mg 现货 Stock Image
G125955-1g
1g 现货 Stock Image

基本描述

别名 加兰他敏 | 加兰他明 | 尼瓦林 | 强肌 | 雪花胺 | 雪花莲胺
英文别名 AKOS015965330 | KBio3_002636 | Lycoremin | NSC-100058 | Spectrum5_001673 | KBioSS_001751 | BDBM10404 | Galantaminum | NCGC00017256-17 | NSC 100058 | Galantamine | DB00674 | AC-20240 | CHEBI:42944 | GALANTAMINE [VANDF] | Galantaminum [INN-Latin] | Jilkon |
规格或纯度 Moligand™, ≥98%
英文名称 Galanthamine
生化机理 加兰他敏是一种选择性乙酰胆碱酯酶抑制剂,可阻断乙酰胆碱的分解,使受体被激活的时间更长。对丁酰胆碱酯酶的选择性超过 50 倍。抑制红细胞胆碱酯酶活性的效力是人脑组织的 10 倍。
储存温度 -20°C储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 乙酰胆碱酯酶抑制剂(卡特赖特血型)
备注 如果有可能,您尽量在使用的当天配置溶液,并在当天使用完它。但是,如果您需要预先配制储备溶液,我们建议您将溶液等份保存在-20°C的密封小瓶中。通常,它们最多可以使用一个月。在使用前和打开样品瓶之前,我们建议您让您的产品在室温下平衡至少1小时。有毒,请参阅SDS以获取更多信息。需要更多关于溶解度,用法和处理的建议吗?请访问我们的常见问题(FAQ)页面以获取更多详细信息。
产品介绍

Galanthamine是长效中枢活性乙酰胆碱酯酶(AChE)抑制剂,IC50为410 nM,同时是神经元烟碱乙酰胆碱受体的变构增强剂。A selective acetylcholinesterase inhibitor

Galanthamine is a long-acting, centrally active acetylcholinesterase(AChE) inhibitor (IC50 = 410 nM) and allosteric potentiator at neuronal nicotinic ACh receptors.
A selective acetylcholinesterase inhibitor

纯度 ≥98%

关联靶点(人)

ACHE Tclin 乙酰胆碱酯酶(Acetylcholinesterase) (33 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
BCHE Tclin 胆碱酯酶(Cholinesterase) (4 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
PDE5A Tclin Phosphodiesterase 5A (5113 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
EGFR Tclin Epidermal growth factor receptor erbB1 (33727 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
F2 Tclin Thrombin (11687 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CA2 Tclin Carbonic anhydrase II (17698 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ESR1 Tclin Estrogen receptor alpha (17718 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HMGCR Tclin HMG-CoA reductase (2475 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NR3C1 Tclin Glucocorticoid receptor (14987 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
INSR Tclin Insulin receptor (5558 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PGR Tclin Progesterone receptor (8562 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRB2 Tclin Beta-2 adrenergic receptor (11824 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM2 Tclin Muscarinic acetylcholine receptor M2 (10671 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRB1 Tclin Beta-1 adrenergic receptor (6630 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR1A Tclin Serotonin 1a (5-HT1a) receptor (14969 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA2A Tclin Alpha-2a adrenergic receptor (9450 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AR Tclin Androgen Receptor (11781 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
VDR Tclin Vitamin D receptor (26531 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ACE Tclin Angiotensin-converting enzyme (1423 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD2 Tclin Dopamine D2 receptor (23596 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAOA Tclin Monoamine oxidase A (11911 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CNR1 Tclin Cannabinoid CB1 receptor (20913 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD1 Tclin Dopamine D1 receptor (9720 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD4 Tchem Dopamine D4 receptor (7907 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ACHE Tclin Acetylcholinesterase (18204 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PTGS1 Tclin Cyclooxygenase-1 (9233 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A2 Tclin Norepinephrine transporter (10102 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HRH2 Tclin Histamine H2 receptor (5428 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA1D Tclin Alpha-1d adrenergic receptor (4171 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR1B Tclin Serotonin 1b (5-HT1b) receptor (2801 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR2A Tclin Serotonin 2a (5-HT2a) receptor (14758 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR2C Tclin Serotonin 2c (5-HT2c) receptor (11471 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADORA1 Tclin Adenosine A1 receptor (17603 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CALCR Tclin Calcitonin receptor (2215 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A4 Tclin Serotonin transporter (12625 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA1A Tclin Alpha-1a adrenergic receptor (8359 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PTGS2 Tclin Cyclooxygenase-2 (13999 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HRH1 Tclin Histamine H1 receptor (7573 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA1B Tclin Alpha-1b adrenergic receptor (2912 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRM1 Tclin Mu opioid receptor (19785 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD3 Tclin Dopamine D3 receptor (14368 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AVPR1A Tclin Vasopressin V1a receptor (5412 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRD1 Tclin Delta opioid receptor (15096 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRK1 Tclin Kappa opioid receptor (16155 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A3 Tclin Dopamine transporter (10535 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
KCNH2 Tclin HERG (29587 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR4 Tclin Serotonin 4 (5-HT4) receptor (2068 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PDE3A Tclin Phosphodiesterase 3A (3309 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ESR2 Tclin Estrogen receptor beta (9272 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYSLTR1 Tclin Cysteinyl leukotriene receptor 1 (2118 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ERBB2 Tclin Receptor protein-tyrosine kinase erbB-2 (7851 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点(其它种属)

Agtr2 Angiotensin II type 2 (AT-2) receptor (803 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mc4r Melanocortin receptor 4 (1205 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Ltc4s Leukotriene C4 synthase (1 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Sigmar1 Sigma opioid receptor (160 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Npy1r Neuropeptide Y receptor type 1 (8 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Cckar Cholecystokinin A receptor (90 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PREP Prolyl endopeptidase (14 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Nos2 Nitric oxide synthase, inducible (3573 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mapk1 MAP kinase ERK2 (650 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mmp9 Matrix metalloproteinase 9 (38 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Klebsiella pneumoniae (43867 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Staphylococcus aureus (210822 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Escherichia coli (133304 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Bacillus subtilis (32866 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Plasmodium falciparum (966862 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Leishmania donovani (89745 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Trypanosoma cruzi (99888 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Felis catus (3858 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mus musculus (284745 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Trypanosoma brucei rhodesiense (7991 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RAW264.7 (28094 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
BCHE Cholinesterase (8742 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Brain (1 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Clk1 Dual specificity protein kinase CLK1 (404 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Cat Catalase (15 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Ache Acetylcholinesterase and butyrylcholinesterase (AChE and BChE) (232 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Glra2 Glycine receptor (1745 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

PubChem SID 504751856
分子类型 小分子
IIUPAC Name (1S,12S,14R)-9-methoxy-4-methyl-11-oxa-4-azatetracyclo[8.6.1.01,12.06,17]heptadeca-6(17),7,9,15-tetraen-14-ol
INCHI 1S/C17H21NO3/c1-18-8-7-17-6-5-12(19)9-14(17)21-16-13(20-2)4-3-11(10-18)15(16)17/h3-6,12,14,19H,7-10H2,1-2H3/t12-,14-,17-/m0/s1
InChi Key ASUTZQLVASHGKV-JDFRZJQESA-N
Smiles CN1CCC23C=CC(CC2OC4=C(C=CC(=C34)C1)OC)O
Isomeric SMILES CN1CC[C@@]23C=C[C@@H](C[C@@H]2OC4=C(C=CC(=C34)C1)OC)O
分子量 287.35
Reaxy-Rn 625778
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=625778&ln=

化学和物理性质

溶解性 Soluble in acetone, chloroform, ethanol (4 mg/ml), DMSO (10 mg/ml), and water (50 mM).
分子量 287.350 g/mol
XLogP3 1.800
氢键供体数Hydrogen Bond Donor Count 1
氢键受体数Hydrogen Bond Acceptor Count 4
可旋转键计数Rotatable Bond Count 1
精确质量Exact Mass 287.152 Da
单同位素质量Monoisotopic Mass 287.152 Da
拓扑极表面积Topological Polar Surface Area 41.900 Ų
重原子数Heavy Atom Count 21
形式电荷Formal Charge 0
复杂度Complexity 440.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 3
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

安全和危险性(GHS)

象形图 GHS06,   GHS07,   GHS08,   GHS09
信号词 Danger

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批号(Lot Number) 证书类型 货号
L2307678 分析证书 G125955
L2307679 分析证书 G125955
L2307680 分析证书 G125955
K2211456 分析证书 G125955
K2211491 分析证书 G125955
K2211451 分析证书 G125955
I2526432 分析证书 G125955
I2526442 分析证书 G125955
K2426193 分析证书 G125955
G1901017 分析证书 G125955

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此产品的引用文献

引用文献

1. Taly A, Corringer PJ, Guedin D, Lestage P, Changeux JP.  (2009)  Nicotinic receptors: allosteric transitions and therapeutic targets in the nervous system..  Nat Rev Drug Discov,  (9): (733-50).  [PMID:19721446]
2. Prvulovic D, Hampel H, Pantel J.  (2010)  Galantamine for Alzheimer's disease..  Expert Opin Drug Metab Toxicol,  (3): (345-54).  [PMID:20113148]
3. Ago Y, Koda K, Takuma K, Matsuda T.  (2011)  Pharmacological aspects of the acetylcholinesterase inhibitor galantamine..  J Pharmacol Sci,  116  (1): (6-17).  [PMID:21498956]
4. Haobin Shi, Yuhong Zheng, Mengyao Wu, Li Fu.  (2019)  Graphene Ink Modified Glassy Carbon Electrode as electrochemical sensor for Galantamine Determination.  International Journal of Electrochemical Science,  14  (1546).  [10.20964/2019.02.56]
5. Jia Song, Jiaying Yu, Kai Sun, Zhixin Chen, Xiaoxiao Xing, Yumeng Yang, Chunyu Sun, Zhifei Wang.  (2023)  Preparation of a Highly Selective “Off-On” Rhodamine-Based Fluorescent Probe for the Specific Determination of Carboxylesterase 2 and Cell Imaging.  ANALYTICAL LETTERS,  56  (15): (2457-2472).  [10.1080/00032719.2023.2175213]
6. Zhixu Chen, Jincai Wang, Jiaming Yuan, Zhen Wang, Zhengchao Tu, Jacques Crommen, Wenhui Luo, Jialiang Guo, Tingting Zhang, Zhengjin Jiang.  (2023)  Rapid screening of neuraminidase inhibitors using an at-line nanofractionation platform involving parallel oseltamivir-sensitive/resistant neuraminidase bioassays.  JOURNAL OF CHROMATOGRAPHY A,  1687  (463693).  [PMID:36516530] [10.1016/j.chroma.2022.463693]
7. Wei Li, Chong Qiao, Jing Pang, Guolin Zhang, Yinggang Luo.  (2019)  The versatile O-methyltransferase LrOMT catalyzes multiple O-methylation reactions in amaryllidaceae alkaloids biosynthesis.  INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES,  141  (680).  [PMID:31494163] [10.1016/j.ijbiomac.2019.09.011]
8. Yu-Mei Zhao, Lv-Huan Wang, Si-Fan Luo, Qi-Qin Wang, Ruin Moaddel, Ting-Ting Zhang, Zheng-Jin Jiang.  (2018)  Magnetic beads-based neuraminidase enzyme microreactor as a drug discovery tool for screening inhibitors from compound libraries and fishing ligands from natural products.  JOURNAL OF CHROMATOGRAPHY A,  1568  (123).  [PMID:30005943] [10.1016/j.chroma.2018.07.031]
9. Lvhuan Wang, Yumei Zhao, Yanyan Zhang, Tingting Zhang, Jeroen Kool, Govert W. Somsen, Qiqin Wang, Zhengjin Jiang.  (2018)  Online screening of acetylcholinesterase inhibitors in natural products using monolith-based immobilized capillary enzyme reactors combined with liquid chromatography-mass spectrometry.  JOURNAL OF CHROMATOGRAPHY A,  1563  (135).  [PMID:29866504] [10.1016/j.chroma.2018.05.069]
10. Lingqi Gao, Junde Han, Jie Bai, Jing Dong, Sen Zhang, Mazhong Zhang, Jijian Zheng.  (2018)  Nicotinic Acetylcholine Receptors are Associated with Ketamine-induced Neuronal Apoptosis in the Developing Rat Retina.  NEUROSCIENCE,  376  (1).  [PMID:29427655] [10.1016/j.neuroscience.2018.01.057]
11. Tingting Cai, Li Zhang, Rong Wang, Chen Liang, Yurong Zhang, Yinlong Guo.  (2013)  Effect of ammonium perfluorooctanoate on acetylcholinesterase activity and inhibition using MALDI-FTICRMS.  INTERNATIONAL JOURNAL OF MASS SPECTROMETRY,  353  (80).  [10.1016/j.ijms.2013.05.011]
12. Chongyang Mu, Mashooq Khan, Jinpeng Liu, Xinfeng Dong, Zhengtong Wang, Ping Song, Qiongzheng Hu, Li Yu.  (2024)  Development of surface droplet evaporation-based sensing platform for screening lipase inhibitors.  MICROCHEMICAL JOURNAL,  205  (111256).  [10.1016/j.microc.2024.111256]

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