| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| ln Vitro |
Arterolane (Trioxolane 7; OZ277; RBx-11160) is an antimalarial medication with IC50 values of 1.1 nM (0.43 ng/mL) for P. falciparum Ro73 and W2, respectively. Arterolane also inhibited several other Plasmodium falciparum species, with IC50 values of 1.0, 1.6, 0.90, 0.91, 1.4, 1.5, 0.83, and 0.84 ng/mL for P. falciparum K1, Fc27, FVO, NF54, HB3, and FCB1. They are ITG2-F6 and MAD20[1], respectively.
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| References | |
| Additional Infomation |
Arterolane is an oxaspiro compound that is dispiro[cyclohexane-1,3'-[1,2,4]trioxolane-5',2''-tricyclo[3.3.1.1(3,7)]decane] substituted by a 2-[(2-amino-2-methylpropyl)amino]-2-oxoethyl group at position 4s. Its maleic acid salt is used as an antimalarial drug in combination with piperaquine. It has a role as an antimalarial and an antiplasmodial drug. It is a member of adamantanes, a secondary carboxamide, a primary amino compound, a trioxolane and an oxaspiro compound. It is a conjugate base of an arterolane(1+).
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| Molecular Formula |
C22H36N2O4
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|---|---|
| Molecular Weight |
392.54
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| Exact Mass |
392.268
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| CAS # |
664338-39-0
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| Related CAS # |
664338-39-0
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| PubChem CID |
10475633
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| Appearance |
White to off-white solid powder
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| Density |
1.202 g/cm3
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| Boiling Point |
572.161ºC at 760 mmHg
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| Flash Point |
299.832ºC
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| LogP |
4.787
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
28
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| Complexity |
598
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VXYZBLXGCYNIHP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H36N2O4/c1-20(2,23)13-24-19(25)12-14-3-5-21(6-4-14)26-22(28-27-21)17-8-15-7-16(10-17)11-18(22)9-15/h14-18H,3-13,23H2,1-2H3,(H,24,25)
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| Chemical Name |
N-(2-Amino-2-methylpropyl)-2-{dispiro[adamantane-2,2'-[1,3,5]trioxolane-4',1''-cyclohexane]-4''-yl}acetamide
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| Synonyms |
RBx 11160RBx11160 RBx-11160 ArterolaneOZ 277OZ-277 OZ277
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~254.76 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (4.25 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 16.7 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: ≥ 1.67 mg/mL (4.25 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 16.7 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: ≥ 1.67 mg/mL (4.25 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 | 2.5475 mL | 12.7376 mL | 25.4751 mL | |
| 5 mM | 0.5095 mL | 2.5475 mL | 5.0950 mL | |
| 10 mM | 0.2548 mL | 1.2738 mL | 2.5475 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03452475 | Completed | Drug: Arterolane-piperaquine Drug: Arterolane-piperaquine+mefloquine |
Plasmodium Falciparum | University of Oxford | March 7, 2018 | Phase 3 |
| NCT02461186 | Withdrawn | Drug: Arterolane maleate-piperaquine phosphate (Synriam) |
Uncomplicated Falciparum Malaria Artemisinin-resistant |
University of Oxford | June 2015 | Phase 2 Phase 3 |
| NCT00362050 | Completed | Drug: Treatment with 3 dose groups of RBx11160 over 7 days |
Plasmodium Falciparum Malaria | Medicines for Malaria Venture | June 2006 | Phase 2 |
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