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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Artelinic acid targets the malaria parasite Plasmodium falciparum. As an artemisinin derivative, it is believed to act on the parasite's digestive vacuole, generating reactive oxygen species that damage parasite proteins and membranes. It is effective against multidrug-resistant strains.
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| ln Vitro |
In vitro, Artelinic acid has antimalarial activity against Plasmodium falciparum. It is a water-soluble artemisinin analogue. Its activity makes it a valuable tool for studying malaria parasite biology and developing new antimalarial therapies.
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| ln Vivo |
In dogs, the elimination time t1/2 for artemisinic acid (10 mg/kg; i.v.) is 0.37 hours, the CL is 14.99 mL/min/kg, the Vss is 9.52 L, and the AUC0–12h is 11219 ng h/mL. 1]. The elimination time t1/2 of artemisinic acid (10 mg/kg; IM) in dogs was 6.14 hours, the CL was 14.58 mL/min/kg, the Vss was 36.1 L, and the AUC0-12h was 96372 ng h/mL. 1]. Artemisinic acid (10 mg/kg; oral) in dogs had an AUC0–12h of 8839 ng h/mL, a CL of 14.6 mL/min/kg, a Vss of 16.2 L, and an elimination time t1/2 of 2.21 hours. 1].
In vivo, Artelinic acid is used for the treatment of multidrug-resistant malaria. As a water-soluble artemisinin analogue, it can be administered parenterally. Its efficacy against multidrug-resistant Plasmodium falciparum has been demonstrated in preclinical and clinical studies. It is a valuable compound for antimalarial research. |
| Enzyme Assay |
In vitro antimalarial assays for Artelinic acid involve measuring its inhibition of Plasmodium falciparum growth. Parasite cultures are treated with increasing concentrations of the compound, and parasite growth is measured by ³H-hypoxanthine incorporation or by microscopy. IC50 values are calculated from dose-response curves.
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| Cell Assay |
For in vitro cell-based assays, Plasmodium falciparum-infected erythrocytes are cultured and treated with Artelinic acid at various concentrations. Parasite growth is monitored by microscopy or flow cytometry. The compound's effects on parasite morphology and metabolism are assessed. Cytotoxicity in mammalian cells is assessed using MTT or standard assays.
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| Animal Protocol |
Animal/Disease Models: 3-5 year old adult male beagle dogs [1]
Doses: 10 mg/kg Route of Administration: intravenous (iv) (iv)injection (pharmacokinetic/PK/PK analysis) Experimental Results: Elimination time t1/2 was 0.37 hrs (hrs (hours)), CL was 14.99 mL/ min/kg, the Vss of dogs is 9.52 L, and the AUC0-12h is 11219 ng h/mL. In vivo animal studies with Artelinic acid are conducted in mouse models of malaria. Mice are infected with Plasmodium berghei or P. falciparum and treated with the compound orally or parenterally. Parasitemia is monitored by blood smears. Survival rates and cure rates are measured. Pharmacokinetic studies assess the compound's distribution, metabolism, and excretion. |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
The known metabolites of β-atenline include dihydroartemisinin (DQHS). Artelinic acid (CAS: 120020-26-0) has a molecular weight of 418.5 g/mol and a molecular formula of C23H30O7. Appearance: solid. Purity: ≥95%. Synonyms: 蒿醚林酸. Storage: room temperature. The compound is a water-soluble artemisinin analogue with antimalarial activity. |
| Toxicity/Toxicokinetics |
Artelinic acid is a research compound and is not approved for human therapeutic use in many regions. In preclinical studies, it has shown a manageable safety profile. As an antimalarial agent, it may have effects on the parasite and host. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
[1]. Li QG, et al. Pharmacology and toxicology of artelinic acid: preclinical investigations on pharmacokinetics, metabolism, protein and red blood cell binding, and acute and anorectic toxicities. Trans R Soc Trop Med Hyg. 1998 May-Jun;92(3):332-40.
[2]. Hartell MG, et al. Nuclear magnetic resonance and molecular modeling analysis of the interaction of the antimalarial drugs artelinic acid and artesunic acid with beta-cyclodextrin. J Pharm Sci. 2004 Aug;93(8):2076-89. |
| Additional Infomation |
Artelinic acid is a water-soluble artemisinin analogue with antimalarial activity against multidrug-resistant Plasmodium falciparum. It has the CAS number 120020-26-0 and a molecular weight of 418.5 g/mol. It holds promise in advancing malaria treatment strategies. It is not FDA-approved and is intended for research use only.
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| Molecular Formula |
C23H30O7
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|---|---|
| Molecular Weight |
418.4801
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| Exact Mass |
418.199
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| CAS # |
120020-26-0
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| PubChem CID |
10341948
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| Appearance |
White to off-white solid powder
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| Vapour Pressure |
2.28E-12mmHg at 25°C
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| LogP |
4.109
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
662
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| Defined Atom Stereocenter Count |
8
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| SMILES |
O1[C@@]23[C@]4([H])O[C@@]([H])([C@]([H])(C([H])([H])[H])[C@]2([H])C([H])([H])C([H])([H])[C@@]([H])(C([H])([H])[H])[C@]3([H])C([H])([H])C([H])([H])[C@@](C([H])([H])[H])(O1)O4)OC([H])([H])C1C([H])=C([H])C(C(=O)O[H])=C([H])C=1[H]
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| InChi Key |
UVNHKOOJXSALHN-ILQPJIFQSA-N
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| InChi Code |
InChI=1S/C23H30O7/c1-13-4-9-18-14(2)20(26-12-15-5-7-16(8-6-15)19(24)25)27-21-23(18)17(13)10-11-22(3,28-21)29-30-23/h5-8,13-14,17-18,20-21H,4,9-12H2,1-3H3,(H,24,25)/t13-,14-,17+,18+,20+,21-,22-,23-/m1/s1
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| Chemical Name |
4-[[(1R,4S,5R,8S,9R,10S,12R,13R)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecan-10-yl]oxymethyl]benzoic acid
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~238.96 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 10 mg/mL (23.90 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 100.0 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: ≥ 10 mg/mL (23.90 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 100.0 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: ≥ 10 mg/mL (23.90 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 | 2.3896 mL | 11.9480 mL | 23.8960 mL | |
| 5 mM | 0.4779 mL | 2.3896 mL | 4.7792 mL | |
| 10 mM | 0.2390 mL | 1.1948 mL | 2.3896 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.
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