A9361
アーテメーター
≥98% (HPLC)
別名:
SM-224, ジヒドロアルテミシニンメチルエステル, ジヒドロキンガオスメチルエステル
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この商品について
実験式（ヒル表記法）:
C16H26O5
CAS番号:
分子量:
298.37
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
51101908
MDL number:
製品名
アーテメーター, ≥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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Biochem/physiol Actions
アーテメーターは、アルテミシニンのメチルエーテル誘導体です。マラリア原虫(Plasmodium falciparum)の多剤耐性菌株に対して使用され、住血吸虫症の治療として有望です。
アーテメーターは、抗マラリア化合物です。
Artemisinin possesses a highly reactive endoperoxide bridge, which is core for its therapeutic potential. The endoperoxide bond reacts with iron in the erythrocytes with malarial parasite. This leads to the generation of reactive oxygen species (ROS) directly targeting the parasite. Artemisinin also regulates ferroptosis in tumor cells. The α cell transcription factor Arx expression is reduced by artemether. Prolonged exposure of primary islets also resulted in loss if identity in endocrine cell types and their functionality.
Application
Artemether has been used:
- as an anti-schistosomal compound to test it effect on the larval stages of S. mansoni
- to sensitize mouse embryonic fibroblasts (MEFs) and human osteosarcoma HT1080 cells to cysteine starvation (STV)-induced ferroptosis
- to stimulate islets and its effect on α to β transdifferentiation
Features and Benefits
This compound was developed by Novartis. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
General description
Artemisinin (ART) is a natural compound present in Artemisia annua, a traditional Chinese plant.
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Org. Perox. D
保管分類
5.2 - Organic peroxides and self-reacting hazardous materials
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Dylan R Pillai et al.
Malaria journal, 11, 131-131 (2012-05-01)
Monitoring resistance phenotypes for Plasmodium falciparum, using in vitro growth assays, and relating findings to parasite genotype has proved particularly challenging for the study of resistance to artemisinins. Plasmodium falciparum isolates cultured from 28 returning travellers diagnosed with malaria were
Urs Duthaler et al.
Veterinary parasitology, 186(3-4), 270-280 (2011-12-31)
The pharmacokinetic (PK) parameters of artesunate, artemether and their metabolites dihydroartemisinin (DHA) and dihydroartemisinin-glucuronide (DHA-glucuronide) were determined in sheep naturally infected with Fasciola hepatica. Sheep were treated either with artesunate (intramuscular (i.m.): 40 and 60 mg/kg) or artemether (i.m.: 40
Abel Nhama et al.
Malaria journal, 13, 309-309 (2014-08-12)
Mozambique adopted artemisinin-based combination therapy (ACT) for the treatment of uncomplicated Plasmodium falciparum malaria in the year 2006, and since 2009 artemether-lumefantrine (AL) and artesunate-amodiaquine (ASAQ) have been proposed as alternative first-line treatments. A multicentre study was conducted in five
S H Xiao et al.
Parasitology today (Personal ed.), 16(3), 122-126 (2000-02-26)
The fight against schistosomiasis in China has been very effective in reducing the number of infections across the country. However, the drug of choice, praziquantel, has no prophylactic effect, which reduces its efficacy in high transmission areas. This situation has
Cong L Yuan et al.
Emerging infectious diseases, 18(1), 125-127 (2012-01-21)
The phylum Apicomplexa comprises intracellular protozoa that include many human pathogens. Their nearest relatives are chromerids and colpodellids. We report a case of a Babesia spp.-like relapsing infection caused by a newly described microorganism related to the Apicomplexa. This case
資料
Bioactive small molecules for immune system signaling target identification/validation and antibiotics, antivirals, and antifungals offered.
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