Artemotil

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.

Product information

CAS Number: 75887-54-6

Molecular Weight: 312.40

Formula: C17H28O5

Synonym:

β-Arteether

(+)-Arteether

Arteether

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

Smiles: C[C@@]12CC[C@H]3[C@H](C)CC[C@H]4[C@@H](C)[C@@H](OCC)O[C@H](O1)[C@]43OO2

InChiKey: NLYNIRQVMRLPIQ-XQLAAWPRSA-N

InChi: InChI=1S/C17H28O5/c1-5-18-14-11(3)13-7-6-10(2)12-8-9-16(4)20-15(19-14)17(12,13)22-21-16/h10-15H,5-9H2,1-4H3/t10-,11-,12+,13+,14+,15-,16-,17-/m1/s1

Technical Data

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

In Vitro:

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.

In Vivo:

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).

References:

1. Dwivedi H, et al. Parasitology. 2016, 143(12):1557-68.

Products are for research use only. Not for human use.