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经验公式(希尔记法):
C16H26O5
化学文摘社编号:
分子量:
298.37
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
51101908
MDL number:
产品名称
蒿甲醚, ≥98% (HPLC)
InChI key
SXYIRMFQILZOAM-HVNFFKDJSA-N
SMILES string
CO[C@H]1OC2O[C@@]3(C)CCC4[C@H](C)CCC([C@H]1C)[C@@]24OO3
InChI
1S/C16H26O5/c1-9-5-6-12-10(2)13(17-4)18-14-16(12)11(9)7-8-15(3,19-14)20-21-16/h9-14H,5-8H2,1-4H3/t9-,10-,11+,12+,13+,14-,15-,16-/m1/s1
assay
≥98% (HPLC)
form
powder
optical activity
[α]/D +155 to +175°, c = 0.5 in methanol
color
off-white to light brown
solubility
DMSO: ≥20 mg/mL
originator
Novartis
storage temp.
room temp
Quality Level
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Application
蒿甲醚已被用于:
- 作为抗血吸虫化合物测试其对幼虫期曼氏血吸虫的作用
- 提高小鼠胚胎成纤维细胞 (MEF) 和人骨肉瘤HT1080 细胞对半胱氨酸饥饿 (STV) 引起的铁死亡的敏感性
- 刺激胰岛及其对α到β分化转移的作用
Biochem/physiol Actions
蒿甲醚是一种抗疟疾化合物。
蒿甲醚是青蒿素的一种甲醚衍生物。它可用于治疗疟疾寄生虫恶性疟原虫的多重耐药菌株,并显示出治疗血吸虫病的潜力。
青蒿素含有具备高反应活性的内过氧化合物桥,这种桥结构是其治疗潜力的核心。内过氧化合物键与疟原虫红细胞中的铁反应。 这导致产生直接靶向疟原虫的活性氧(ROS)。 青蒿素还可调节肿瘤细胞中的铁死亡。α蒿甲醚可减少细胞转录因子Arx 的表达。初生胰岛的长期暴露还会导致难以鉴定内分泌细胞类型及其功能。
General description
青蒿素 (ART) 是一种存在于传统中草药青蒿中的天然化合物。
wgk
WGK 3
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Org. Perox. D
存储类别
5.2 - Organic peroxides and self-reacting hazardous materials
flash_point_f
Not applicable
flash_point_c
Not applicable
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The arsenal in anthelminthic treatment against schistosomiasis is limited and relies almost exclusively on a single drug, praziquantel (PZQ). Thus, resistance to PZQ could constitute a major threat. Even though PZQ is potent in killing adult worms, its activity against
Shuhua Xiao et al.
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Two decades ago, a group of Chinese scientists discovered the antischistosomal properties of artemether, a derivative of the antimalarial drug artemisinin. However, it was only recently that the importance of this finding was recognized internationally, following a collaborative effort between
Dominic Mosha et al.
Antimicrobial agents and chemotherapy, 58(8), 4583-4592 (2014-05-29)
Artemether-lumefantrine (AL) is the first-line treatment for uncomplicated malaria in the second and third trimesters of pregnancy. Its efficacy during pregnancy has recently been challenged due to altered pharmacokinetic (PK) properties in this vulnerable group. The aim of this study
J Utzinger et al.
Current medicinal chemistry, 8(15), 1841-1860 (2002-01-05)
Human schistosomiasis, a chronic and debilitating parasitic disease of the tropics, is ranked second after malaria in terms of public health importance. At present, there is no vaccine available, and chemotherapy is the cornerstone of schistosomiasis control. Praziquantel is the
Bart M J De Spiegeleer et al.
Journal of pharmaceutical and biomedical analysis, 70, 111-116 (2012-07-10)
During the stability evaluation of β-artemether containing finished drug products, a consistent and disproportional increase in the UV-peak areas of β-artemether degradation products, when compared to the peak area decline of β-artemether itself, was observed. This suggested that the response
商品
Bioactive small molecules for immune system signaling target identification/validation and antibiotics, antivirals, and antifungals offered.
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