Artelinic acid
Based on 1 Customer Validation
Artelinic acid, a derivative of Artemisinin, is an antimalarial agent for the treatment of multidrug resistant strains of Plasmodium falciparum. Artelinic acid can be administered by various routes of administration, including intravenous, intramuscular and oral routes.
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- Purity: 98.14%
- CAS No.: 120020-26-0
- 화학식: C23H30O7
- 분자량:418.48
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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Plasmodium |
Artelinic acid (10 mg/kg; intramuscular) has an elimination time t1/2 of 6.14 hours, a CL of 14.58 mL/min/kg, a Vss of 36.1 L and a AUC0-12h of 96372 ng h/mL for dogs[1].
Artelinic acid (10 mg/kg; oral) has an elimination time t1/2 of 2.21 hours, a CL of 14.6 mL/min/kg, a Vss of 16.2 L and a AUC0-12h of 8839 ng h/mL for dogs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male beagle dogs 3-5 years old[1]
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Dosage:10 mg/kg
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Administration:i.v. (Pharmacokinetic Analysis)
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Result:Had an elimination time t1/2 of 0.37 hours, a CL of 14.99 mL/min/kg, a Vss of 9.52 L and a AUC0-12h of 11219 ng h/mL for dogs.
Chemical Information
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CAS No. 120020-26-0
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Appearance Solid
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분자량 418.48
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화학식 C23H30O7
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Color White to off-white
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SMILES
O=C(O)C1=CC=C(CO[C@@H]2[C@H](C)[C@]3([H])CC[C@@H](C)[C@]4([H])CC[C@@](O5)(C)OO[C@]43[C@]5([H])O2)C=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (238.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 10 mg/mL (23.90 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 10 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 10 mg/mL (23.90 mM); Clear solution
This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3896 mL | 11.9480 mL | 23.8960 mL | 59.7400 mL |
| 5 mM | 0.4779 mL | 2.3896 mL | 4.7792 mL | 11.9480 mL | |
| 10 mM | 0.2390 mL | 1.1948 mL | 2.3896 mL | 5.9740 mL | |
| 15 mM | 0.1593 mL | 0.7965 mL | 1.5931 mL | 3.9827 mL | |
| 20 mM | 0.1195 mL | 0.5974 mL | 1.1948 mL | 2.9870 mL | |
| 25 mM | 0.0956 mL | 0.4779 mL | 0.9558 mL | 2.3896 mL | |
| 30 mM | 0.0797 mL | 0.3983 mL | 0.7965 mL | 1.9913 mL | |
| 40 mM | 0.0597 mL | 0.2987 mL | 0.5974 mL | 1.4935 mL | |
| 50 mM | 0.0478 mL | 0.2390 mL | 0.4779 mL | 1.1948 mL | |
| 60 mM | 0.0398 mL | 0.1991 mL | 0.3983 mL | 0.9957 mL | |
| 80 mM | 0.0299 mL | 0.1494 mL | 0.2987 mL | 0.7468 mL | |
| 100 mM | 0.0239 mL | 0.1195 mL | 0.2390 mL | 0.5974 mL |
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