1. Anti-infection
  2. Parasite
  3. Artemotil

Artemotil (Synonyms: β-Arteether; (+)-Arteether; Arteether)

Cat. No.: HY-B0770 Purity: >98.0%
Handling Instructions

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.

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Artemotil Chemical Structure

Artemotil Chemical Structure

CAS No. : 75887-54-6

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Description

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[1][2].

IC50 & Target

IC50: 1.61 nM (Plasmodium falciparum malaria)[1]

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[1].

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)[2].

Animal Model: Sprague-Dawley male rats (220-280 g)[2]
Dosage: 25 mg/kg; 1 mL/kg body weight
Administration: Intravenous injection; daily; for 7 days
Result: Anorectic toxicity was observed, and that caused significant reductions in food consumption and body weight after day 2.
Molecular Weight

312.40

Formula

C₁₇H₂₈O₅

CAS No.

75887-54-6

SMILES
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Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (160.05 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2010 mL 16.0051 mL 32.0102 mL
5 mM 0.6402 mL 3.2010 mL 6.4020 mL
10 mM 0.3201 mL 1.6005 mL 3.2010 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.00 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (8.00 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.00 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: >98.0%

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Artemotil
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HY-B0770
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