| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
| Targets |
Heme polymerization in Plasmodium falciparum (inhibition of heme polymerase), with additional effects on nucleic acid synthesis, protein synthesis, and glycolysis. The precise molecular target is not fully defined, but the downstream consequence is accumulation of cytotoxic free heme.
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|---|---|
| ln Vitro |
It has been demonstrated that quinidine sulfate, an antiarrhythmic medication, effectively blocks numerous classes of K+ channels in a variety of cell types via influencing ionic currents in the myocardium [1]. Ik peak amplitude decreases in a dose-dependent manner when quinidine sulfate is applied in a bath. It is calculated that at 0 mV, the Kd for Ik blockage is 41 μM [1]. The rate of Ik decay is increased by quinidine sulfate in a dose-dependent manner, and membrane depolarization amplifies this action. Quinidine sulfate also lengthens the half-life of recovery from inactivation and induces a 5 mV hyperpolarizing change in the steady-state inactivation curve. When evaluated at -30 mV, quinidine sulfate had no effect on the beginning of inactivation [1].
Quinine sulfate inhibits P. falciparum growth in vitro, with IC50 values dependent on the parasite strain and assay method (typically in the nanomolar to low-micromolar range). It is active against chloroquine-sensitive and some chloroquine-resistant strains, though resistance is widespread. |
| ln Vivo |
Quinidine sulfate is quickly absorbed; 60 to 90 minutes after oral dosing, the plasma concentration reaches its peak. Other salts, such as polygalacturonate and gluconate, have lower peak concentrations and are absorbed more slowly [2]. About 70–90% of quinidine sulfate is linked to plasma proteins. In the liver, it goes through oxidative metabolism to produce N-oxide, 3-hydroxy, O-desmethyl, and 2'-quinidinone [2]. Rats' metabolism of amphetamine is inhibited by quinidine sulfate. Quinidine sulfate pretreatment led to a large rise in amphetamine excretion to 542% of control levels during 24 and 48 hours, coupled by a significant decrease in parahydroxyamphetamine excretion to 7.2 and 24.1% of vehicle control levels at 24 and 48 hours, respectively. [3].
Quinine sulfate is a clinically established antimalarial drug used for severe and uncomplicated malaria. In animal models, it reduces parasitemia and improves survival in Plasmodium-infected rodents and primates. Its pharmacokinetics and toxicity are well characterized in humans. |
| Enzyme Assay |
In vitro assays measure inhibition of heme polymerization or parasite growth. Heme polymerization can be assessed by spectrophotometric or radiolabeled heme precipitation assays. Parasite growth inhibition is measured by [³H]-hypoxanthine incorporation or SYBR Green-based DNA quantification in P. falciparum cultures.
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| Cell Assay |
In vitro cell-based assays culture P. falciparum (e.g., 3D7 or Dd2 strains) in human erythrocytes under standard conditions. Compound is added at serial dilutions, and after 48–72 hours, parasitemia is quantified by flow cytometry, microscopy, or lactate dehydrogenase assay. IC50 values are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal experiments use Plasmodium berghei or P. yoelii-infected mice. Quinine sulfate is administered intraperitoneally or orally at doses guided by pharmacokinetic studies. Efficacy is assessed by parasitemia reduction, survival time extension, and cure rate compared with vehicle-treated controls.
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| References | |
| Additional Infomation |
Quinine sulfate is the sulfate form of quinine, an alkaloid isolate of quinidine. Quinine has multiple mechanisms of action, including reducing oxygen uptake and carbohydrate metabolism; interfering with DNA replication and transcription through DNA insertion; and reducing muscle fiber excitability by altering calcium distribution. This drug can also inhibit the drug efflux pump P-glycoprotein, which is overexpressed in multidrug-resistant tumors and may therefore enhance the efficacy of certain antitumor drugs. (NCI04)
Quinine is an alkaloid extracted from the bark of the cinchona tree. It is used as an antimalarial drug and is the active ingredient in cinchona extracts, which have been used for malaria treatment since before 1633. Quinine is also a mild antipyretic and analgesic, and has been used to treat the common cold. It was once widely used as a bittering agent and flavoring agent and is still used to treat babesiosis. Quinine is also effective against certain muscle disorders, particularly nocturnal leg cramps and congenital myotonia, because it acts directly on muscle cell membranes and sodium channels. The mechanism of its antimalarial effect is not fully understood. |
| Molecular Formula |
C20H24N2O2.H2O4S
|
|---|---|
| Molecular Weight |
422.49524
|
| Exact Mass |
746.335
|
| CAS # |
549-56-4
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| Related CAS # |
Quinine;130-95-0;Quinine hydrobromide;549-49-5
|
| PubChem CID |
11949689
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
1136.7ºC at 760mmHg
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| Flash Point |
641.2ºC
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| LogP |
6.65
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| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
29
|
| Complexity |
538
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
C=C[C@H]1C[N@](CC[C@H]1C2)[C@@H]2[C@H](O)C3=CC=NC4=CC=C(OC)C=C34.O=S(O)(O)=O
|
| InChi Key |
AKYHKWQPZHDOBW-DSXUQNDKSA-N
|
| InChi Code |
InChI=1S/C20H24N2O2.H2O4S/c1-3-13-12-22-9-7-14(13)10-19(22)20(23)16-6-8-21-18-5-4-15(24-2)11-17(16)18;1-5(2,3)4/h3-6,8,11,13-14,19-20,23H,1,7,9-10,12H2,2H3;(H2,1,2,3,4)/t13-,14-,19-,20+;/m0./s1
|
| Chemical Name |
(R)-[(2S,4S,5R)-5-ethenyl-1-azabicyclo[2.2.2]octan-2-yl]-(6-methoxyquinolin-4-yl)methanol;sulfuric acid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: ~5 mg/mL (~11.8 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (5.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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: ≥ 0.5 mg/mL (1.18 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 DMSO stock solution (5.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: 0.5 mg/mL (1.18 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Suspended solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (5.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3669 mL | 11.8343 mL | 23.6686 mL | |
| 5 mM | 0.4734 mL | 2.3669 mL | 4.7337 mL | |
| 10 mM | 0.2367 mL | 1.1834 mL | 2.3669 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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