Artemotil (β-Arteether) has antimalarial activity for the treatment of chloroquine-resistant Plasmodium falciparum malaria with an IC50 of 1.61 nM. Artemotil also has central nervous system (CNS) neurotoxicity and anorectic toxicity in rats, dogs and monkeys.
CAS Number: 75887-54-6
Molecular Weight: 312.40
Chemical Name: (1R,4S,5R,8S,9R,10S,12R,13R)-10-ethoxy-4,8,12-trihydrogenio-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.0⁴,¹³.0⁸,¹³]hexadecane
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 50 mg/mL (160.05 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
The antimalarial activity of Artemotil is test in vitro against chloroquine-resistant and chloroquine-sensitive Plasmodium falciparum parasites. The mean 50% inhibitory concentration (IC50) for Artemotil is 1.61 nM (range 1.57-1.92 nM). Artemotil is approximately 2.5-fold more potent than artemisinin.
Artemotil treatment (25 mg/kg; intravenous injection; daily; for 7 days; Sprague-Dawley male rats) shows anorectic toxicity and causes significant reductions in food consumption and body weight after day 2. AUC on day 7 is 5-fold higher than AUC on day 1. The elimination t1/2 of Artemotil is also prolonged from 13.7 hours (day 1) to 31.2 hours (day 7).
- Dwivedi H, et al. Parasitology. 2016, 143(12):1557-68.
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