| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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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].
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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. |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Beta-artelinic acid has known human metabolites that include Dihydroqinghaosu (DQHS). |
| 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. |
| Molecular Formula |
C23H30O7
|
|---|---|
| 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
|
| 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]
|
| 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
|
| 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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