1. Immunology/Inflammation GPCR/G Protein Anti-infection
  2. CXCR Parasite
  3. Artemotil

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

Cat. No.: HY-B0770 Purity: ≥98.0%
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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.

For research use only. We do not sell to patients.

Artemotil Chemical Structure

Artemotil Chemical Structure

CAS No. : 75887-54-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 61 In-stock
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Solid
5 mg USD 55 In-stock
10 mg USD 88 In-stock
25 mg USD 150 In-stock
50 mg USD 225 In-stock
100 mg USD 330 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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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

Plasmodium

 

Cellular Effect
Cell Line Type Value Description References
Ehrlich IC50
13.1 μM
Compound: 4
Cytotoxicity against mouse EAC after 3 days by MTT assay
Cytotoxicity against mouse EAC after 3 days by MTT assay
[PMID: 8350087]
HUVEC IC50
> 50 μM
Compound: 13
Inhibitory activity against human umbilical vein endothelial cells (HUVEC) was assayed using MTT colorimetric proliferation assay
Inhibitory activity against human umbilical vein endothelial cells (HUVEC) was assayed using MTT colorimetric proliferation assay
[PMID: 14552753]
Vero CC50
136057 nM
Compound: Arteether
Cytotoxicity against african green monkey Vero C1008 cells after 72 hrs by MTT assay
Cytotoxicity against african green monkey Vero C1008 cells after 72 hrs by MTT assay
[PMID: 23270565]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@H]1[C@@](CC[C@@H](C)[C@]2([H])CC[C@]3(C)O4)([H])[C@@]2(OO3)[C@]4([H])O[C@@H]1OCC

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : 50 mg/mL (160.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.08 mg/mL (6.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: 2.08 mg/mL (6.66 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: ≥98.0%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2010 mL 16.0051 mL 32.0102 mL 80.0256 mL
5 mM 0.6402 mL 3.2010 mL 6.4020 mL 16.0051 mL
10 mM 0.3201 mL 1.6005 mL 3.2010 mL 8.0026 mL
15 mM 0.2134 mL 1.0670 mL 2.1340 mL 5.3350 mL
20 mM 0.1601 mL 0.8003 mL 1.6005 mL 4.0013 mL
25 mM 0.1280 mL 0.6402 mL 1.2804 mL 3.2010 mL
30 mM 0.1067 mL 0.5335 mL 1.0670 mL 2.6675 mL
40 mM 0.0800 mL 0.4001 mL 0.8003 mL 2.0006 mL
50 mM 0.0640 mL 0.3201 mL 0.6402 mL 1.6005 mL
60 mM 0.0534 mL 0.2668 mL 0.5335 mL 1.3338 mL
80 mM 0.0400 mL 0.2001 mL 0.4001 mL 1.0003 mL
100 mM 0.0320 mL 0.1601 mL 0.3201 mL 0.8003 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Artemotil
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