Artemisinin (Qinghaosu; NSC 369397)

Alias: qinghaosu; NSC-369397; NSC369397; NSC 369397;also known as qinghaosu

Cat No.:V5119 Purity: ≥98%

COA Product Data Instructions for use SDS

Artemisinin (Qinghaosu; NSC 369397) Chemical Structure CAS No.: 63968-64-9
Product category: HCV

This product is for research use only, not for human use. We do not sell to patients.

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Other Forms of Artemisinin (Qinghaosu; NSC 369397):

Artemisinin-d3 (Qinghaosu-d3; NSC 369397-d3)

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Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

HPLC

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Biological Data

Product Description

Artemisinin (also known as qinghaosu in Chinese; NSC-369397), discovered by Tu Youyou (2015 Nobel Prize winner in Medicine) team, is a naturally occurring anti-malarial drug isolated from the aerial parts of Artemisia annua L. plants. Artemisinin and its semi-synthetic derivatives are a group of drugs that possess the most rapid action of all current drugs against Plasmodium falciparum malaria.

Biological Activity I Assay Protocols (From Reference)

Targets

Plasmodium

ln Vitro

Artemisinin (3.125-100 μM) concentration-dependently suppresses Aβ25-35 induced cytotoxicity in PC12 cells. Artemisinin (25 μM) suppresses Aβ25-35-induced LDH release, apoptosis and ROS production, attenuates Aβ-induced mitochondrial membrane potential loss and caspase 3/7 activity increase, and stimulates the phosphorylation of ERK1/2 in a time- and concentration-dependent manner in PC12 cell. ERK 1/2 pathway mediates the protect effects of artemisinin in PC12 cells[1]. Artemisinin shows cytotoxic activity in MCF-7/Dox cell line with IC50 of 3.7±0.4 μg/mL after 24 h treatment. Besides, Artemisinin treatment of MCF-7 cells, sensitive and resistant to Dox and DDP, causes a decrease in expression of proteins such as LF, FTH1, and HEP. Artemisinin activates p38 MAPK-kinase cascade regardless of the oxidative stress due to inhibition of VEGF expression and cell migration[2]. Artemisinin (50, 100 or 200 mg) significantly inhibits isoflurane-induced hippocampal neuronal loss, decreases caspase-3-positive cell counts and also cleaves caspase-3 expression, and modulates the expression of apoptosis pathway proteins. Artemisinin modulates JNK/ERK 1/2 signalling and histone acetylation[3]. Artemisinin inhibits HCV replication in a dose-dependent manner with EC50 value of 167±38 µM. Artemisinin and its most potent analogues partially inhibit the in vitro replication of HCV by induction of reactive oxygen species (ROS)[4]. Artemisinin significantly inhibits VSMC proliferation in a dose-dependent manner. Artemisinin (1 mM) for 72 h significantly reduces the expression of proliferating cell nuclear antigen messenger RNA[5].

ln Vivo

Artemisinin (50, 100 or 200 mg/kg b.wt/day, p.o.) prevents isoflurane-induced working memory impairments as observed in T-maze test. Artemisinin enhances spatial navigation and memory of rats exposed to isoflurane. Artemisinin-treated rats exhibit markedly better performance in comparison with isoflurane-alone-exposed rats[3].

Cell Assay

For this purpose, cells are cultivated in 96-well plates in DMEM, supplemented with insulin. The artemisinin, Dox, and DDP are added to media at different concentrations and the cells are cultivated for either 24 or 48 h. For this purpose artemisinin is diluted in 0.01% DMSO in media. After this time, 10 µL of the MTT dye solution (5 mg/mL in phosphate buffer saline) is added to the cells; the cells are incubated at the same conditions for 3 h. After centrifugation (1500 rpm, 5 min) the supernatant is removed. 100 μL of dimethyl sulfoxide is added to each well, to dissolve formazan. The absorption is measured, using a multi-well spectrophotometer at a wavelength of 540 nm.

Animal Protocol

Separate group of rat pups (total rat pups 80; n = 16 per group) is administered artemisinin (50, 100 or 200 mg/kg body weight) via oral gavage, every day from P2 to P21. On P7, the pups are exposed to isoflurane (0.75% in 30% oxygen or air) for 6 h in a temperature-controlled chamber. Animals that are not exposed to anaesthesia nor given artemisinin served as control group, while rats that receive isoflurane alone are grouped as anaesthetic-controls.

References

[1]. Artemisinin protects PC12 cells against β-amyloid-induced apoptosis through activation of the ERK1/2 signaling pathway. Redox Biol. 2017 Apr 4;12:625-633.

[2]. Artemisinin Prevents Glutamate-Induced Neuronal Cell Death Via Akt Pathway Activation. Front Cell Neurosci. 2018 Apr 20;12:108.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C15H22O5
Molecular Weight	282.3322
Exact Mass	282.15
Elemental Analysis	C, 63.81; H, 7.85; O, 28.33
CAS #	63968-64-9
Related CAS #	Artemisinin-d3;176652-07-6
Appearance	Solid powder
SMILES	O=C1[C@H](C)[C@]2([H])CC[C@@H](C)[C@]3([H])CC[C@@](O4)(C)OO[C@]32[C@]4([H])O1
InChi Key	BLUAFEHZUWYNDE-NNWCWBAJSA-N
InChi Code	InChI=1S/C15H22O5/c1-8-4-5-11-9(2)12(16)17-13-15(11)10(8)6-7-14(3,18-13)19-20-15/h8-11,13H,4-7H2,1-3H3/t8-,9-,10+,11+,13-,14-,15-/m1/s1
Chemical Name	(3R,5aS,6R,8aS,9R,12S,12aR)-3,6,9-trimethyloctahydro-12H-3,12-epoxy[1,2]dioxepino[4,3-i]isochromen-10(3H)-one
Synonyms	qinghaosu; NSC-369397; NSC369397; NSC 369397;also known as qinghaosu
HS Tariff Code	2934.99.9001
Storage	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)	DMSO : 50~56 mg/mL (177.10~198.34 mM) H2O : < 0.1 mg/mL
Solubility (In Vivo)	Solubility in Formulation 1: ≥ 2.08 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More Solubility in Formulation 3: ≥ 2.08 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 4: 3% DMSO+ 97% Corn oil: 6mg/ml (21.25mM) (Please use freshly prepared in vivo formulations for optimal results.)

Solubility (In Vitro)

DMSO : 50~56 mg/mL (177.10~198.34 mM)
H2O : < 0.1 mg/mL

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

View More

Solubility in Formulation 3: ≥ 2.08 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

Solubility in Formulation 4: 3% DMSO+ 97% Corn oil: 6mg/ml (21.25mM)

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.5420 mL	17.7098 mL	35.4195 mL
	5 mM	0.7084 mL	3.5420 mL	7.0839 mL
	10 mM	0.3542 mL	1.7710 mL	3.5420 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

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g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

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Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Biological Data

Artemisinin concentration-dependently suppressed Aβ25-35-induced cell viability lose in PC12 cells. [1].Redox Biol. 2017 Apr 4;12:625-633.
Artemisinin suppressed Aβ25-35-induced LDH release and apoptosis in PC12 cells. [1].Redox Biol. 2017 Apr 4;12:625-633.
Artemisinin reduced the increase of Aβ25-35-induced oxidative stress in PC12 cells.[1].Redox Biol. 2017 Apr 4;12:625-633.
Artemisinin attenuated Aβ-induced mitochondrial membrane potential (△ψm) loss and caspase 3/7 activity increase in PC12 cells. [1].Redox Biol. 2017 Apr 4;12:625-633.
Artemisinin stimulated the phosphorylation of ERK1/2 in a time- and concentration-dependent manner in PC12 cells. [1].Redox Biol. 2017 Apr 4;12:625-633.
ERK 1/2 pathway mediated the protect effects of artemisinin in PC12 cells.[1].Redox Biol. 2017 Apr 4;12:625-633.