Artemisinin ADC Cytotoxin inhibitor

Cat.No.S1282

Artemisinin is a sesquiterpene endoperoxide which is a potent antimalarial agent.
Artemisinin ADC Cytotoxin inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 282.33

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 282.33 Formula

C15H22O5

Storage (From the date of receipt)
CAS No. 63968-64-9 Download SDF Storage of Stock Solutions

Synonyms Qinghaosu, NSC 369397 Smiles CC1CCC2C(C(=O)OC3C24C1CCC(O3)(OO4)C)C

Solubility

In vitro
Batch:

DMSO : 57 mg/mL (201.89 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 24 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

In vitro

Artemisinin's antimalarial activity has been shown to be mediated by activated oxygen (i.e., superoxide, hydrogen peroxide, and/or hydroxyl radicals). This compound and heroin appear to be forming an adduct whose behavior resembles the behavior of the parasite this compound product. [1] Its activity can be potentiated by oxygen and oxidizing agents and attenuated by reducing agents. This compound susceptibility can be influenced by genetic changes in the loci encoding P. falciparum multidrug resistance protein 1 (PfMDR1) and P. falciparum CHQ resistance transporter (PfCRT). [2] It is effective not only against multi-resistant strains of P. falciparum, but have broad stage specificity against the Plasmodium life cycle including activity throughout the asexual blood stages and also the sexual gametocyte stages which may reduce the spread of the disease in areas of low transmission. This chemical has also been investigated for its antiproliferative effects against a wide range of cancer cell lines. It is active against other parasite species such as Toxoplasma and Babesia that do not contain hematin. This compound results in decreased proliferation, increased levels of oxidative stress, induction of apoptosis and inhibition of angiogenesis in cancer cells. It has also been shown to inhibit the falcipains, a papain family cysteine protease that aid hemoglobin degradation. [3]

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05750459 Recruiting
Plasmodium Falciparum Infection
National Institute of Allergy and Infectious Diseases (NIAID)
November 29 2023 Phase 4
NCT05343312 Active not recruiting
Malaria
Centro de Investigacao em Saude de Manhica|United States Agency for International Development (USAID)
March 16 2022 Phase 4

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