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| Other Sizes |
| ln Vitro |
In the human liver cancer HepG2 cell line, quinine sulfate hydrate (150 μM, 30 minutes) suppresses the growth and cytostatic effects of dengue virus [1]. In the human liver cancer HepG2 cell line, quinine sulfate hydrate (37.5-150 μM, 24 hours) dramatically lowers viral DENV RNA and protein levels in a dose-dependent manner [1].
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| ln Vivo |
There is a certain inhibitory effect of quinine sulfate hydrate (oral gavage, 12 or 15 mg/kg, weekly, 16 weeks) on Swiss albino mice skin cancer [2]. The antioxidant defense system, which includes SOD, CAT, and GSH enzyme activities, will decline in the testicular tissue of male adult albino rats given quinine sulfate hydrate (oral gavage, 10 mg/kg, daily, for 8 weeks) [3].
|
| Cell Assay |
Cell proliferation assay [1]
Cell Types: Human hepatoma cell line (HepG2) Tested Concentrations: 150 μM Incubation Duration: 30 minutes Experimental Results: Compared with untreated, DENV virus replication was inhibited and the yield reached 19%. diminished DENV-positive cells from 23.28% to 12.05% in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: Swiss albino mice 7-8 weeks (weight 24 grams) [2]
Doses: 12 mg/kg, 15 mg/kg Route of Administration: po (oral gavage); weekly; 16-week Experimental Results: 12 mg/kg dose Tumor size and weight were Dramatically diminished at 15 mg/kg, with little effect at higher doses of 15 mg/kg. |
| References |
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| Additional Infomation |
Quinine Sulfate is the sulfate salt form of the quinidine alkaloid isolate quinine. Quinine has many mechanisms of action, including reduction of oxygen intake and carbohydrate metabolism; disruption of DNA replication and transcription via DNA intercalation; and reduction of the excitability of muscle fibers via alteration of calcium distribution. This agent also inhibits the drug efflux pump P-glycoprotein which is overexpressed in multi-drug resistant tumors and may improve the efficacy of some antineoplastic agents. (NCI04)
An alkaloid derived from the bark of the cinchona tree. It is used as an antimalarial drug, and is the active ingredient in extracts of the cinchona that have been used for that purpose since before 1633. Quinine is also a mild antipyretic and analgesic and has been used in common cold preparations for that purpose. It was used commonly and as a bitter and flavoring agent, and is still useful for the treatment of babesiosis. Quinine is also useful in some muscular disorders, especially nocturnal leg cramps and myotonia congenita, because of its direct effects on muscle membrane and sodium channels. The mechanisms of its antimalarial effects are not well understood. See also: Quinine Sulfate (annotation moved to). |
| Molecular Formula |
C20H28N2O7S
|
|---|---|
| Molecular Weight |
440.51
|
| Exact Mass |
782.356
|
| CAS # |
6119-70-6
|
| Related CAS # |
Quinine hydrochloride dihydrate;6119-47-7;Quinine;130-95-0;Quinine hemisulfate;804-63-7;Quinine hydrobromide;549-49-5
|
| PubChem CID |
16211610
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
495.9ºC at 760 mmHg
|
| Melting Point |
233-235ºC
|
| Flash Point |
253.7ºC
|
| LogP |
6.521
|
| Hydrogen Bond Donor Count |
6
|
| Hydrogen Bond Acceptor Count |
14
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
55
|
| Complexity |
538
|
| Defined Atom Stereocenter Count |
8
|
| SMILES |
COC1=CC2=C(C=CN=C2C=C1)[C@H]([C@@H]3C[C@@H]4CCN3C[C@@H]4C=C)O.COC1=CC2=C(C=CN=C2C=C1)[C@H]([C@@H]3C[C@@H]4CCN3C[C@@H]4C=C)O.O.O.OS(=O)(=O)O
|
| InChi Key |
ZHNFLHYOFXQIOW-LPYZJUEESA-N
|
| InChi Code |
InChI=1S/2C20H24N2O2.H2O4S.2H2O/c2*1-3-13-12-22-9-7-14(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;;/h2*3-6,8,11,13-14,19-20,23H,1,7,9-10,12H2,2H3;(H2,1,2,3,4);2*1H2/t2*13-,14-,19-,20+;;;/m00.../s1
|
| Chemical Name |
(1R)-(6-methoxyquinolin-4-yl)((2S,4S,5R)-5-vinylquinuclidin-2-yl)methanol hemisulfate hydrate
|
| Synonyms |
Chinini sulfas Quinine hemisulfate salt monohydrate Quinine sulfate dihydrate
|
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2701 mL | 11.3505 mL | 22.7010 mL | |
| 5 mM | 0.4540 mL | 2.2701 mL | 4.5402 mL | |
| 10 mM | 0.2270 mL | 1.1350 mL | 2.2701 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 |
| NCT01289561 | COMPLETED | Drug: Alcohol + Caffeine Beverage Drug: Alcohol + Caffeine-placebo |
Alcohol or Other Drugs Effects | Johns Hopkins University | 2011-01 | Phase 1 |
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