| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg | |||
| Other Sizes |
| Targets |
The primary therapeutic target of Artemisic acid is the malaria parasite Plasmodium species, against which it disrupts cellular function. As a precursor to artemisinin, its antimalarial mechanism is ultimately linked to the endoperoxide bridge formed during synthesis, which generates reactive oxygen species that damage the parasite. Beyond antimalarial applications, it exhibits antibacterial activity, anti-adipogenic effects through reduced expression of C/EBPδ and PPARγ, and anti-mycobacterial activity. Artemisinic acid also decreases triglyceride levels and glycerol-3-phosphate dehydrogenase (GPDH) activity in human adipose tissue-derived mesenchymal stem cells (hAMSCs).
|
|---|---|
| ln Vitro |
In vitro, Artemisic acid demonstrates antibacterial activity and is active against different bacteria and certain fungal species. It exhibits anti-adipogenic effects in hAMSCs at concentrations of 50-400 µM, decreasing triglyceride levels and GPDH activity in a dose-dependent manner, and inhibits adipocyte differentiation at 200 µM. It also shows anti-mycobacterial potency with a reported MIC of 250 µg/mL, which is superior to artemisinin's 1000 µg/mL. Antimalarial activity has been reported with an IC50 of approximately 62-78 µM, though an IC50 greater than 175 µM has also been noted in some studies.
|
| ln Vivo |
In vivo, Artemisic acid has demonstrated antipyretic effects and serves as the biosynthetic precursor to artemisinin, which is clinically used as an antimalarial agent. As a precursor, its in vivo efficacy against malaria is realized through conversion to artemisinin or related derivatives. The compound also shows anti-adipogenesis effects in vivo through modulation of adipocyte differentiation pathways. However, detailed in vivo pharmacokinetic and pharmacodynamic data for Artemisic acid itself, independent of its role as a precursor, remain limited in publicly available literature.
|
| Enzyme Assay |
For cell-free enzyme assays involving Artemisic acid, typical protocols include enzyme inhibition studies using purified targets such as HMG-CoA reductase or other metabolic enzymes. The compound's role as a precursor in artemisinin synthesis can be studied using in vitro enzymatic conversion assays with cytochrome P450 enzymes that catalyze the oxidation of artemisinic acid to artemisinin. Antimicrobial activity can be assessed via standard broth microdilution methods to determine minimum inhibitory concentration (MIC) values against bacterial or fungal strains.
|
| Cell Assay |
In vitro cellular activity is assessed using standard cell lines such as hAMSCs for anti-adipogenic studies. Cells are treated with serial dilutions of Artemisic acid (e.g., 50-400 µM) and endpoints include triglyceride level measurement, glycerol-3-phosphate dehydrogenase (GPDH) activity assays, and analysis of adipocyte differentiation markers such as C/EBPδ and PPARγ expression via Western blot or qPCR. Cytotoxicity and antiproliferative effects can be evaluated using MTT or SRB assays in cancer cell lines to assess anti-tumor activity.
|
| Animal Protocol |
In vivo efficacy is evaluated in animal models of malaria (e.g., Plasmodium-infected mice) or inflammation. As a precursor to artemisinin, Artemisic acid can be administered via oral gavage or intraperitoneal injection, and endpoints include parasitemia reduction, survival rate, and inflammatory biomarker analysis. For anti-adipogenic studies, rodent models of obesity or metabolic syndrome may be used, with endpoints including body weight, adipose tissue mass, and serum lipid profiles.
|
| ADME/Pharmacokinetics |
DMSO solubility: 60-100 mg/mL; in vivo formulation: 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline (≥2.5 mg/mL). Molecular weight: 234.33 g/mol; molecular formula: C15H22O2. Density: 1.5±0.1 g/cm³. Powder stable at -20°C for 3 years, 4°C for 2 years; in solvent at -80°C for 6 months, -20°C for 1 month.
|
| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available. As a natural sesquiterpene from Artemisia annua, it is generally considered to have low toxicity, but standard safety pharmacology and toxicology studies (e.g., acute toxicity in rodents, Ames test for genotoxicity, hERG assay for cardiotoxicity) would be required for drug development. Some studies indicate that concentrations exceeding 175 µM may be required to observe significant effects.
|
| References | |
| Additional Infomation |
(+)-Artemisinic acid is a monocarboxylic acid with the structure of a 2-enoic acid, substituted at the 2-position with a 4,7-dimethyl-1,2,3,4,4a,5,6,8a-octahydronaphth-1-yl group (1S,4R,4aS,8aR diastereomers). It is the sesquiterpene precursor of artemisinin, extracted from Artemisia annua. It is a metabolite. It is a monocarboxylic acid, a carbon-bicyclic compound, a sesquiterpene, and a member of the octahydronaphthyl group. Functionally, it is related to (+)-artemisinol. It is the conjugate acid of (+)-artemisinic acid ester. Artemisinic acid has been reported to exist in Artemisia annua, Artemisia carvifolia, and other organisms with relevant data.
Artemisic acid is a research-grade compound, not approved for therapeutic use. It is primarily used as a reference standard, a starting material for the semi-synthesis of artemisinin and related derivatives, and a subject of investigation for its intrinsic biological properties. No clinical trials or FDA approval have been reported for Artemisic acid itself; it remains in preclinical research stages. Its mechanism includes antimalarial activity through disruption of Plasmodium cellular function and anti-adipogenic effects via regulation of C/EBPδ and PPARγ expression. |
| Molecular Formula |
C₁₅H₂₂O₂
|
|---|---|
| Molecular Weight |
234.33
|
| Exact Mass |
234.161
|
| CAS # |
80286-58-4
|
| PubChem CID |
10922465
|
| Appearance |
White to off-white solid powder
|
| Density |
1.0±0.1 g/cm3
|
| Boiling Point |
373.6±11.0 °C at 760 mmHg
|
| Melting Point |
129-131℃
|
| Flash Point |
273.3±10.2 °C
|
| Vapour Pressure |
0.0±1.8 mmHg at 25°C
|
| Index of Refraction |
1.505
|
| LogP |
5.11
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
17
|
| Complexity |
367
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
C[C@@H]1CC[C@H]([C@@H]2[C@H]1CCC(=C2)C)C(=C)C(=O)O
|
| InChi Key |
PLQMEXSCSAIXGB-SAXRGWBVSA-N
|
| InChi Code |
InChI=1S/C15H22O2/c1-9-4-6-12-10(2)5-7-13(14(12)8-9)11(3)15(16)17/h8,10,12-14H,3-7H2,1-2H3,(H,16,17)/t10-,12+,13+,14+/m1/s1
|
| Chemical Name |
2-[(1R,4R,4aS,8aR)-4,7-dimethyl-1,2,3,4,4a,5,6,8a-octahydronaphthalen-1-yl]prop-2-enoic acid
|
| Synonyms |
Arteannuic acid Artemisinic acid Qing Hao acid
|
| 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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~426.75 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (3.54 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 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 0.83 mg/mL (3.54 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 8.3 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: ≥ 0.83 mg/mL (3.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2675 mL | 21.3374 mL | 42.6749 mL | |
| 5 mM | 0.8535 mL | 4.2675 mL | 8.5350 mL | |
| 10 mM | 0.4267 mL | 2.1337 mL | 4.2675 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.
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.
(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.