| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| Targets |
CaMK III Plasmodium
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|---|---|
| ln Vitro |
Camiquine succinate (24–48 hours) disrupts protein synthesis, produces irregularities in trophozoites, and prevents the formation of trophozoites and fragmented aggregates in the parasite [1]. With EC50 = 1.0 nM, EC90 = 2.4 nM, and EC99 = 5.9 nM against 3D7 parasites, carbaquine succinate exhibits good efficacy[1]. When coupled with hepatocytes or liver microsomes, camelquin succinate shows good metabolic stability [1].
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| ln Vivo |
Cabamiquine (DDD107498) exhibits an ED90 of 0.57 mg/kg after a single oral dose in mice infected with the rodent parasite P. berghei[1].
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| References |
[1]. Baragaña B, et al. A novel multiple-stage antimalarial agent that inhibits protein synthesis. Nature. 2015 Jun 18;522(7556):315-20.
[2]. Baragaña B, et al. Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy. J Med Chem. 2016 Nov 10;59(21):9672-9685. |
| Molecular Formula |
C31H37FN4O6
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|---|---|
| Molecular Weight |
580.65
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| CAS # |
2444781-71-7
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| Related CAS # |
Cabamiquine;1469439-69-7
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| SMILES |
FC1C([H])=C([H])C2=C(C=1[H])C(=C([H])C(C1C([H])=C([H])C(=C([H])C=1[H])C([H])([H])N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H])=N2)C(N([H])C([H])([H])C([H])([H])N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H])=O.O([H])C(C([H])([H])C([H])([H])C(=O)O[H])=O
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| Solubility (In Vitro) |
DMSO : 135 mg/mL (232.50 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.25 mg/mL (3.87 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 22.5 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: ≥ 2.25 mg/mL (3.87 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 22.5 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: ≥ 2.25 mg/mL (3.87 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 | 1.7222 mL | 8.6110 mL | 17.2221 mL | |
| 5 mM | 0.3444 mL | 1.7222 mL | 3.4444 mL | |
| 10 mM | 0.1722 mL | 0.8611 mL | 1.7222 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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