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Artemether (SM-224)

Catalog No.
A4014
Semi-synthetic derivative of artemisinin
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$50.00
In stock
100mg
$50.00
In stock

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Background

Artemether is a semi-synthetic derivative of artemisinin (qinghaosu), a naturally occurring peroxide lactone derived from a traditional Chinese herbal remedy Artemisia annua L., to enhance the solubility and antimalarial activity of its parental compound. Artemether exhibits potent antimalarial and antischistosomal activities against malarial parasites and Schistosoma japonicum infections. Although it has not been well elucidated, an endoperoxide bridge within the chemical structure of Artemether might be the key characteristic considered to be responsible for its antimalarial and antischistosomal activities, which can be metabolized by malarial or schistosomal parasites, under in vivo conditions, generating detrimental oxygen radicals to attack parasite macromolecules.

Reference

Xiao Shuhua and Brian A. Catto.  In vitro and in vivo studies of the effect of artemether on Schistosoma mansoni. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY 1989, 1557-1562

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt298.4
Cas No.71963-77-4
FormulaC16H26O5
Solubilityinsoluble in H2O; ≥15.3 mg/mL in DMSO; ≥90.2 mg/mL in EtOH
Chemical Name(3R,5aS,6R,8aS,9R,10S,12R,12aR)-10-methoxy-3,6,9-trimethyldecahydro-3H-3,12-epoxy[1,2]dioxepino[4,3-i]isochromene
SDFDownload SDF
Canonical SMILES[H][[email protected]]12[[email protected]@]3([[email protected]@]4([H])CC[[email protected]@]2([H])C)[[email protected]@](O[[email protected]](OC)[[email protected]@]4(C)[H])([H])O[[email protected]@](OO3)(C)CC1
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Protocol

Animal experiment [1]:

Animal models

Rat C6 Orthotopic Brain Gliomas Model

Dosage form

33.3mg/kg, 50mg/kg, 66.6mg/kg (p.o.), once a day for 10 days

Application

Compared with the untreated control group, artemether-treated rat C6 glioma primary tumor growth rate and mean tumor volume data indicate that artemether has an inhibitory effect on tumor growth. Within the concentration range used (33.3-66.6 mg / kg daily), artemether has a dose-dependent inhibition of tumor mass in the C6 glioma model in vivo, and co-administration with ferrous sulfate may have effects on animals with tumor synergistic inhibition.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Wu ZP, Gao CW, Wu YG, Zhu QS, Yan Chen, Xin Liu, Chuen Liu. Inhibitive effect of artemether on tumor growth and angiogenesis in the rat C6 orthotopic brain gliomas model. Integr Cancer Ther. 2009 Mar;8(1):88-92. doi:10.1177/1534735408330714. Epub 2009 Jan 27. Erratum in: Integr Cancer Ther. 2009 Jun;8(2):195. PubMed PMID: 19174507.

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