Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: = 99.77%
Targets |
Mitochondrial electron transport
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ln Vitro |
Antimalarial 14 (Compound N3) (zero-400 μM, 48 hours) has a minimal cytotoxic effect on human cells and inhibits Plasmodium falciparum [1]. Plasmodium falciparum's mitochondrial membrane potential is inhibited by antimalarial drug 14 with an IC50ΔΨmit of 16 μM [1].Anti-malarial activity was assessed in vitro for a series of 3-alkyl-2-hydroxy-1,4-naphthoquinones (N1-N5) evaluating the parasitaemia after 48 hours of incubation. Potential cytotoxicity in HEK293T cells was assessed using the MTT assay. Changes in mitochondrial membrane potential of Plasmodium were measured using the fluorescent dye Mitrotracker Red CMXROS [1].
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Enzyme Assay |
Changes in mitochondrial membrane potential (ΨΔmit)[1]
Loss of parasite mitochondrial membrane potential (ΨΔmit) was determined using 5 μM Mitrotracker Red CMXROS as described previously [18]. Cultures were incubated for 30 min at 37°C with the dye and then for 1 h with 10-fold serial dilutions (0.001-100 μM) of N3 and atovaquone. As a control, 5 μM cyanide m-chlorophenylhydrazone (CCCP), a protonophore that dissipate the membrane potential, was used. Results were analysed by flow cytometry as described above. |
Cell Assay |
Cytotoxicity assay[1]
Cell Types: Plasmodium falciparum and HEK293T Tested Concentrations: 0.128, 0.64, 3.2, 16, 80 and 400 μM Incubation Duration: 48 hrs (hours) Experimental Results: demonstrated inhibitory effect against Plasmodium falciparum with IC50 of 443 nM and Exhibits a cytotoxic CC50 of 54.6 ± 0.23 μM. |
Animal Protocol |
3D7 strain parasites were cultured and synchronized as described previously. Briefly, parasites were routinely maintained in A+ human erythrocytes (1-3% parasitaemia and 2% haematocrit) in RPMI-1640 media supplemented with 0.2% sodium bicarbonate, 50 mg/L hypoxanthine and 10% type A+ human serum in 92% N2, 5% CO2 and 3% O2.
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References |
[1]. Schuck DC, et al. Biological evaluation of hydroxynaphthoquinones as anti-malarials. Malar J. 2013 Jul 10;12:234.
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Molecular Formula |
C16H10O3
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Molecular Weight |
250.249
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Exact Mass |
250.063
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CAS # |
1150-59-0
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Appearance |
Yellow to brown solid
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LogP |
2.5
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tPSA |
54.4Ų
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SMILES |
C1=CC=C(C2C(=O)C(=O)C3=CC=CC=C3C=2O)C=C1
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InChi Key |
HCKUADBGJIXWTR-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C16H10O3/c17-14-11-8-4-5-9-12(11)15(18)16(19)13(14)10-6-2-1-3-7-10/h1-9,17H
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Chemical Name |
2-hydroxy-3-phenylnaphthalene-1,4-dione
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Synonyms |
NSC102533; NSC 102533; NSC-102533
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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: ~125 mg/mL (499.5 mM)
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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 | 3.9960 mL | 19.9800 mL | 39.9600 mL | |
5 mM | 0.7992 mL | 3.9960 mL | 7.9920 mL | |
10 mM | 0.3996 mL | 1.9980 mL | 3.9960 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.