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青蒿琥酯

半合成青蒿素衍生物
23篇引用文献
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货号 (SKU) 包装规格 是否现货 价格 数量
A107818-5g
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A107818-25g
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A107818-100g
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Anti-infection (2825) Apoptosis (1467) Ferroptosis (208) JAK/STAT Signaling (505) Parasite (431) STAT (139) Stem Cell/Wnt (1018) 六元杂环化合物 (1702) 病毒蛋白酶 (106) 稠环四氢吡喃类 (14)
main product photo

基本描述

别名 青蒿脂
英文别名 4-oxo-4-{[(1R,4S,5R,8S,9R,10S,12R,13R)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.0?,(1)(3).0?,(1)(3)]hexadecan-10-yl]oxy}butanoic acid | ARTESUNATE [WHO-DD] | NCGC00164600-15 | Q707939 | ARTESUNATE [WHO-IP] | HY-N0193 | UNII-60W3249T9M | 4-oxo
规格或纯度 Moligand™, ≥98%
英文名称 Artesunate
生化机理 半合成青蒿素（Asc-1308）衍生物。诱导血管内皮细胞凋亡。在体内显示抗血管生成和抗寄生虫作用。口服具有活性
应用 青蒿琥酯是一种半合成的青蒿素衍生物,它被证明有效抗寄生虫，如肝吸虫（liver flukes），也显示了对不同类型的肿瘤细胞株有细胞毒性作用。
储存温度 2-8°C储存
运输条件 冰袋运输
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。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

Artesunate is a derivative of artemisinin and belongs to a class with antimicrobial properties. The compound is an active ingredient in the Chinese herb Artemisia annua and has been used in Malaria studies. Artesunate has been tested against 55 cell lines and demonstrated anti-cancer activity. Research shows that conditional expression of CDC25A heightens the sensitivity of tumor cells to artesunate.青蒿琥酯是一种半合成的青蒿素衍生物,它被证明有效抗寄生虫，如肝吸虫（liver flukes），也显示了对不同类型的肿瘤细胞株有细胞毒性作用。

Artesunate is a derivative of artemisinin and belongs to a class with antimicrobial properties. The compound is an active ingredient in the Chinese herb Artemisia annua and has been used in Malaria studies. Artesunate has been tested against 55 cell lines and demonstrated anti-cancer activity. Research shows that conditional expression of CDC25A heightens the sensitivity of tumor cells to artesunate.
A derivative of artemisinin

AI解读

产品属性

ALogP 2.5

关联靶点（人）

ABL1 Tclin Tyrosine-protein kinase ABL (18331 活性数据)
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ESR1 Tclin Estrogen receptor alpha (17718 活性数据)
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NR3C1 Tclin Glucocorticoid receptor (14987 活性数据)
活性类型 Relation Activity value Units Action Type Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal PubMed Id doi Assay Aladdin ID
AR Tclin Androgen Receptor (11781 活性数据)
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CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 活性数据)
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TOP1 Tclin DNA topoisomerase I (7553 活性数据)
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DRD2 Tclin Dopamine D2 receptor (23596 活性数据)
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GABRA1 Tclin GABA receptor alpha-1 subunit (399 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAOA Tclin Monoamine oxidase A (11911 活性数据)
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CNR1 Tclin Cannabinoid CB1 receptor (20913 活性数据)
活性类型 Relation Activity value Units Action Type Journal 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 Journal PubMed Id doi Assay Aladdin ID
ACHE Tclin Acetylcholinesterase (18204 活性数据)
活性类型 Relation Activity value Units Action Type Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal PubMed Id doi Assay Aladdin ID
AVPR2 Tclin Vasopressin V2 receptor (2912 活性数据)
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ADORA1 Tclin Adenosine A1 receptor (17603 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AGTR1 Tclin Type-1 angiotensin II receptor (5176 活性数据)
活性类型 Relation Activity value Units Action Type Journal 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 Journal 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 Journal PubMed Id doi Assay Aladdin ID
PTGS2 Tclin Cyclooxygenase-2 (13999 活性数据)
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HRH1 Tclin Histamine H1 receptor (7573 活性数据)
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OPRM1 Tclin Mu opioid receptor (19785 活性数据)
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DRD3 Tclin Dopamine D3 receptor (14368 活性数据)
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AVPR1A Tclin Vasopressin V1a receptor (5412 活性数据)
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OPRD1 Tclin Delta opioid receptor (15096 活性数据)
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OPRK1 Tclin Kappa opioid receptor (16155 活性数据)
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HTR3A Tclin Serotonin 3a (5-HT3a) receptor (3366 活性数据)
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SLC6A3 Tclin Dopamine transporter (10535 活性数据)
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GRIN1 Tclin Glutamate (NMDA) receptor subunit zeta 1 (122 活性数据)
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KCNH2 Tclin HERG (29587 活性数据)
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CACNA1C Tclin Voltage-gated L-type calcium channel alpha-1C subunit (766 活性数据)
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PDE3A Tclin Phosphodiesterase 3A (3309 活性数据)
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SLC29A1 Tclin Equilibrative nucleoside transporter 1 (1711 活性数据)
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ADRA2B Tclin Alpha-2b adrenergic receptor (4412 活性数据)
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ADRA2C Tclin Alpha-2c adrenergic receptor (4876 活性数据)
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CHRM3 Tclin Muscarinic acetylcholine receptor M3 (7750 活性数据)
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HTR2B Tclin Serotonin 2b (5-HT2b) receptor (10323 活性数据)
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TBXA2R Tclin Thromboxane A2 receptor (5717 活性数据)
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EDNRA Tclin Endothelin receptor ET-A (5008 活性数据)
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ADORA2A Tclin Adenosine A2a receptor (16305 活性数据)
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ADORA3 Tchem Adenosine A3 receptor (15931 活性数据)
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关联靶点（其它种属）

Histidine-rich protein (528 活性数据)
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Npy1r Neuropeptide Y receptor type 1 (8 活性数据)
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Cckar Cholecystokinin A receptor (90 活性数据)
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Pde4d Phosphodiesterase 4D (4 活性数据)
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Mapk1 MAP kinase ERK2 (650 活性数据)
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Hdac6 Histone deacetylase 6 (222 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Trypanosoma brucei brucei (13300 活性数据)
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Plasmodium falciparum (966862 活性数据)
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Schistosoma japonicum (780 活性数据)
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Fasciola hepatica (191 活性数据)
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Candida albicans (78123 活性数据)
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Leishmania donovani (89745 活性数据)
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Trypanosoma cruzi (99888 活性数据)
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Toxoplasma gondii (4585 活性数据)
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Plasmodium berghei (192651 活性数据)
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Plasmodium yoelii (6656 活性数据)
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Schistosoma mansoni (6170 活性数据)
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Human betaherpesvirus 5 (5122 活性数据)
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Mus musculus (284745 活性数据)
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Rattus norvegicus (775804 活性数据)
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Hepatitis B virus (7925 活性数据)
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Plasmodium yoelii nigeriensis (1119 活性数据)
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CHO (4503 活性数据)
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Vero (26788 活性数据)
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L6 (7924 活性数据)
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H22 (575 活性数据)
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Hemozoin (239 活性数据)
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Chuk Inhibitor of nuclear factor kappa-B kinase subunit alpha (16 活性数据)
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rep Replicase polyprotein 1ab (378 活性数据)
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Ikbkb Inhibitor of nuclear factor kappa-B kinase subunit beta (81 活性数据)
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BCHE Cholinesterase (8742 活性数据)
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Plasmodium malariae (15 活性数据)
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Plasmodium vinckei petteri (380 活性数据)
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Plasmodium vivax (152 活性数据)
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Echinococcus multilocularis (18 活性数据)
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TUBB2B Tubulin (2175 活性数据)
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SARS-CoV-2 (38078 活性数据)
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Plasmodium vinckei (20 活性数据)
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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

分子类型 小分子
IUPAC Name 4-oxo-4-[[(1R,4S,5R,8S,9R,10S,12R,13R)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecan-10-yl]oxy]butanoic acid
INCHI InChI=1S/C19H28O8/c1-10-4-5-13-11(2)16(23-15(22)7-6-14(20)21)24-17-19(13)12(10)8-9-18(3,25-17)26-27-19/h10-13,16-17H,4-9H2,1-3H3,(H,20,21)/t10-,11-,12+,13+,16-,17-,18-,19-/m1/s1
InChi Key FIHJKUPKCHIPAT-AHIGJZGOSA-N
Canonical SMILES CC1CCC2C(C(OC3C24C1CCC(O3)(OO4)C)OC(=O)CCC(=O)O)C
Isomeric SMILES C[C@@H]1CC[C@H]2[C@H]([C@@H](O[C@H]3[C@@]24[C@H]1CC[C@](O3)(OO4)C)OC(=O)CCC(=O)O)C
PubChem CID 6917864
分子量 384.42
Reaxy-Rn 6003212

化学和物理性质

溶解性 Soluble in DMSO (25 mg/mL), and ethanol (25 mg/mL).solubility acetone: 33.4 mg/mL.
密度 1.31
敏感性 对热敏感
比旋光度 5.5° (C=1,CH2Cl2)
熔点 133°C
分子量 384.400 g/mol
XLogP3 2.500
氢键供体数Hydrogen Bond Donor Count 1
氢键受体数Hydrogen Bond Acceptor Count 8
可旋转键计数Rotatable Bond Count 5
精确质量Exact Mass 384.178 Da
单同位素质量Monoisotopic Mass 384.178 Da
拓扑极表面积Topological Polar Surface Area 101.000 Ų
重原子数Heavy Atom Count 27
形式电荷Formal Charge 0
复杂度Complexity 623.000
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 8
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）

Reaxy-Rn 6003212
Merck Index 818

 SDS英文版

技术规格说明书

Purity(Neutralization titration) 98-100（%）
Specific Rotation [a]20/D(c=1 in CH2Cl2) 4.5-6.5（°）
Melting point 132-137（℃）
Purity(HPLC) 98-100（%）
Appearance（A107818) White to Off-White Powder
Proton NMR spectrum Conforms to Structure
Solubility in Acetone，Colorless,Clear to Slightly Hazy,1 g + 29.9 mL pass

 技术规格说明书

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找到6个结果

批号(Lot Number) 证书类型 日期 货号
E2305312 分析证书 23-01-11 A107818
E2305613 分析证书 23-01-11 A107818
G2328047 分析证书 23-01-11 A107818
B2219326 分析证书 21-12-30 A107818
B2219341 分析证书 21-12-30 A107818
B2219525 分析证书 21-12-30 A107818

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12. Sennan Qiao, Hansi Zhang, Fei Sun, Zhenyan Jiang.  (2021)  Molecular Basis of Artemisinin Derivatives Inhibition of Myeloid Differentiation Protein 2 by Combined in Silico and Experimental Study.  MOLECULES,  26  (18): (5698).  [PMID:34577169] [10.3390/molecules26185698]
13. Miaomiao Long, Jiamin Xu, Wenjie Fang, Jing Mao, Jie Zhang, Shenhuan Liu, Lipeng Qiu.  (2021)  Enhanced delivery of artesunate by stimuli-responsive polymeric micelles for lung tumor therapy.  JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY,  66  (102812).  [10.1016/j.jddst.2021.102812]
14. Fereja Shemsu Ligani, Fang Zhongying, Li Ping, Guo Jinhan, Fereja Tadesse Haile, Chen Wei.  (2021)  “Turn-off” sensing probe based on fluorescent gold nanoclusters for the sensitive detection of hemin.  ANALYTICAL AND BIOANALYTICAL CHEMISTRY,  413  (6): (1639-1649).  [PMID:33483839] [10.1007/s00216-020-03126-1]
15. Mengqi Bai, Li Qiang, Minjia Meng, Binrong Li, Suao Wang, Yilin Wu, Li Chen, Jiangdong Dai, Yan Liu, Jianming Pan.  (2021)  Upper surface imprinted membrane prepared by magnetic guidance phase inversion method for highly efficient and selective separation of Artemisinin.  CHEMICAL ENGINEERING JOURNAL,  405  (126899).  [10.1016/j.cej.2020.126899]
16. Huang Ming-Zhi, Zhuang Yong, Ning Xu, Zhang Hao, Shen Zhi-Min, Shang Xian-Wen.  (2020)  Artesunate inhibits osteoclastogenesis through the miR-503/RANK axis.  BIOSCIENCE REPORTS,  40  (7): [PMID:32542308] [10.1042/BSR20194387]
17. Yilin Wu, Wendong Xing, Minjia Meng, Jian Lu, Faguang Ma, Jia Gao, Xinyu Lin, Chao Yu.  (2020)  Multiple-functional molecularly imprinted nanocomposite membranes for high-efficiency selective separation applications: An imitated core-shell TiO2@PDA-based MIMs design.  COMPOSITES PART B-ENGINEERING,  198  (108123).  [10.1016/j.compositesb.2020.108123]
18. Zhu Wang, Qianqian Wang, Tao He, Wen Li, Yan Liu, Yuan Fan, Yanping Wang, Qi Wang, Jie Chen.  (2020)  The combination of artesunate and carboplatin exerts a synergistic anti-tumour effect on non-small cell lung cancer.  CLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY,  47  (6): (1083-1091).  [PMID:32072678] [10.1111/1440-1681.13287]
19. Peng Ji, Haiqin Huang, Shirui Yuan, Le Wang, Siqi Wang, Yiwei Chen, Na Feng, Hanitrarimalala Veroniaina, Ziheng Wu, Zhenghong Wu, Xiaole Qi.  (2019)  ROS-Mediated Apoptosis and Anticancer Effect Achieved by Artesunate and Auxiliary Fe(II) Released from Ferriferous Oxide-Containing Recombinant Apoferritin.  Advanced Healthcare Materials,  8  (23): (1900911).  [PMID:31701665] [10.1002/adhm.201900911]
20. Renjie Xu, Ting Han, Li Shen, Jianguo Zhao, Xiang’an Lu.  (2019)  Solubility Determination and Modeling for Artesunate in Binary Solvent Mixtures of Methanol, Ethanol, Isopropanol, and Propylene Glycol + Water.  JOURNAL OF CHEMICAL AND ENGINEERING DATA,  64  (2): (755–762).  [10.1021/acs.jced.8b00988]
21. Yao Yuyuan, Guo Qinglong, Cao Yue, Qiu Yangmin, Tan Renxiang, Yu Zhou, Zhou Yuxin, Lu Na.  (2018)  Artemisinin derivatives inactivate cancer-associated fibroblasts through suppressing TGF-β signaling in breast cancer.  JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH,  37  (1): (1-14).  [PMID:30477536] [10.1186/s13046-018-0960-7]
22. Ting Li, Qingwen Zeng, Xingming Chen, Guojiang Wang, Haiqing Zhang, Aihua Yu, Hairui Wang, Yang Hu.  (2018)  The therapeutic effect of artesunate on rosacea through the inhibition of the JAK/STAT signaling pathway.  Molecular Medicine Reports,  17  (6): (8385-8390).  [PMID:29693177] [10.3892/mmr.2018.8887]
23. Hailong Huang, Xianghui Wang, Hao Ge, Min Xu.  (2016)  Multifunctional Magnetic Cellulose Surface-Imprinted Microspheres for Highly Selective Adsorption of Artesunate.  ACS Sustainable Chemistry & Engineering,  4  (6): (3334–3343).  [10.1021/acssuschemeng.6b00386]

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26. Miaomiao Long, Jiamin Xu, Wenjie Fang, Jing Mao, Jie Zhang, Shenhuan Liu, Lipeng Qiu.  (2021)  Enhanced delivery of artesunate by stimuli-responsive polymeric micelles for lung tumor therapy.  JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY,  66  (102812).  [10.1016/j.jddst.2021.102812]
27. Fereja Shemsu Ligani, Fang Zhongying, Li Ping, Guo Jinhan, Fereja Tadesse Haile, Chen Wei.  (2021)  “Turn-off” sensing probe based on fluorescent gold nanoclusters for the sensitive detection of hemin.  ANALYTICAL AND BIOANALYTICAL CHEMISTRY,  413  (6): (1639-1649).  [PMID:33483839] [10.1007/s00216-020-03126-1]
28. Mengqi Bai, Li Qiang, Minjia Meng, Binrong Li, Suao Wang, Yilin Wu, Li Chen, Jiangdong Dai, Yan Liu, Jianming Pan.  (2021)  Upper surface imprinted membrane prepared by magnetic guidance phase inversion method for highly efficient and selective separation of Artemisinin.  CHEMICAL ENGINEERING JOURNAL,  405  (126899).  [10.1016/j.cej.2020.126899]
29. Huang Ming-Zhi, Zhuang Yong, Ning Xu, Zhang Hao, Shen Zhi-Min, Shang Xian-Wen.  (2020)  Artesunate inhibits osteoclastogenesis through the miR-503/RANK axis.  BIOSCIENCE REPORTS,  40  (7): [PMID:32542308] [10.1042/BSR20194387]
30. Yilin Wu, Wendong Xing, Minjia Meng, Jian Lu, Faguang Ma, Jia Gao, Xinyu Lin, Chao Yu.  (2020)  Multiple-functional molecularly imprinted nanocomposite membranes for high-efficiency selective separation applications: An imitated core-shell TiO2@PDA-based MIMs design.  COMPOSITES PART B-ENGINEERING,  198  (108123).  [10.1016/j.compositesb.2020.108123]
31. Zhu Wang, Qianqian Wang, Tao He, Wen Li, Yan Liu, Yuan Fan, Yanping Wang, Qi Wang, Jie Chen.  (2020)  The combination of artesunate and carboplatin exerts a synergistic anti-tumour effect on non-small cell lung cancer.  CLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY,  47  (6): (1083-1091).  [PMID:32072678] [10.1111/1440-1681.13287]
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33. Renjie Xu, Ting Han, Li Shen, Jianguo Zhao, Xiang’an Lu.  (2019)  Solubility Determination and Modeling for Artesunate in Binary Solvent Mixtures of Methanol, Ethanol, Isopropanol, and Propylene Glycol + Water.  JOURNAL OF CHEMICAL AND ENGINEERING DATA,  64  (2): (755–762).  [10.1021/acs.jced.8b00988]
34. Yao Yuyuan, Guo Qinglong, Cao Yue, Qiu Yangmin, Tan Renxiang, Yu Zhou, Zhou Yuxin, Lu Na.  (2018)  Artemisinin derivatives inactivate cancer-associated fibroblasts through suppressing TGF-β signaling in breast cancer.  JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH,  37  (1): (1-14).  [PMID:30477536] [10.1186/s13046-018-0960-7]
35. Ting Li, Qingwen Zeng, Xingming Chen, Guojiang Wang, Haiqing Zhang, Aihua Yu, Hairui Wang, Yang Hu.  (2018)  The therapeutic effect of artesunate on rosacea through the inhibition of the JAK/STAT signaling pathway.  Molecular Medicine Reports,  17  (6): (8385-8390).  [PMID:29693177] [10.3892/mmr.2018.8887]
36. Hailong Huang, Xianghui Wang, Hao Ge, Min Xu.  (2016)  Multifunctional Magnetic Cellulose Surface-Imprinted Microspheres for Highly Selective Adsorption of Artesunate.  ACS Sustainable Chemistry & Engineering,  4  (6): (3334–3343).  [10.1021/acssuschemeng.6b00386]

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