| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 100mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Plasmodium
Warangalone targets multiple cellular pathways. It inhibits the growth of Plasmodium falciparum parasites, with IC50s of 4.8 μg/mL for the chloroquine-sensitive strain 3D7 and 3.7 μg/mL for the chloroquine-resistant strain K1. It is a powerful inhibitor of protein kinase A (cAK) with an IC50 of 3.5 μM. It also shows anti-inflammatory activity on phospholipase A2-induced paw edema and TPA-induced ear edema in mice. |
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| ln Vitro |
Warangalone is an anti-malarial substance that has the ability to stop the growth of parasite strains 3D7, which is sensitive to chloroquine, and K1, which is resistant to it, with IC50 values of 4.8 μg/mL and 3.7 μg/mL, respectively[1]. With an IC50 of 3.5 μM, warangalone can also inhibit the catalytic subunit of cyclic AMP-dependent protein kinase (cAK)[2]. In comparison to controls, warangalone (30 μM) significantly reduces (8%) the viability of HL-60 cells after 24 hours of exposure. Additionally, warangalone exhibits time-dependent inhibition of HL-60 cell growth within 24 hours. After treating cells with warangalone, there is a time-dependent increase in caspase-9 activity[3].
In vitro, Warangalone inhibits the growth of both strains of Plasmodium falciparum parasite 3D7 (chloroquine sensitive) and K1 (chloroquine resistant) with IC50s of 4.8 μg/mL and 3.7 μg/mL, respectively. It inhibits cyclic AMP-dependent protein kinase catalytic subunit (cAK) with an IC50 of 3.5 μM. When HL-60 cells are exposed to Warangalone (30 μM) for 24 hours, it induces a significant decrease (8%) in cell viability compared to controls. It also inhibits HL-60 cell growth within 24 hours in a time-dependent fashion. A time-dependent increase in caspase-9 activity is observed in Warangalone-treated cells. |
| ln Vivo |
In vivo, Warangalone shows marked effectiveness as an anti-inflammatory on the phospholipase A2-induced paw edema and on the TPA-induced ear edema in mice, after systemic and local administration, respectively. As an anti-malarial compound, it has demonstrated activity against both chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum.
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| Enzyme Assay |
The caspase fluorometric assay kit is used to measure the enzyme activities of caspase-3 and caspase-9. In 24-well plates, cells are seeded at a density of 3×106 cells per well. Following the designated duration of exposure to Warangalone, the cells undergo three PBS washes before being lysed for ten minutes on ice in a lysis buffer. Using a Micro BCA reagent, the protein content of the cell lysates is measured. 50 μg of protein-containing cell lysates are incubated for one hour at 37°C with either a caspase-9 fluorogenic substrate (LEHD-AFC) or a caspase-3 fluorogenic substrate (DEVD-AFC). Fluorometric detection is used to quantify caspase activity[3].
The protein kinase A inhibition assay for Warangalone involves incubating the compound with the catalytic subunit of PKA, ATP, and a peptide substrate. The reaction is carried out in a kinase buffer at 30°C for a specified time. The incorporation of [³²P] into the substrate is measured by scintillation counting. IC50 values are calculated from dose-response curves. |
| Cell Assay |
Cell Titer 96 Aqueous assay kit is used to determine cell viability. A density of 1×105 cells per well is seeded in 96-well plates. Following a 24-hour period at 37°C, 30 μM of warangalone is added to the culture medium. At the designated times, MTS solution is added to the 96-well plates, and the cells are then incubated for one hour at 37°C. A microplate counter is used to measure the absorbance at 490 nm in wavelength[3].
To evaluate the cellular activity of Warangalone, cancer cell lines (such as HL-60 human leukemia cells) are seeded in culture plates and treated with varying concentrations of Warangalone. Cell viability is measured using MTT or trypan blue exclusion assays. Apoptosis is assessed by measuring caspase-9 activity and other apoptotic markers. Cell growth is monitored over time to assess time-dependent effects. |
| Animal Protocol |
The in vivo anti-inflammatory activity of Warangalone is evaluated in mouse models of inflammation. Phospholipase A2-induced paw edema is induced by injection of PLA2 into the mouse paw, and Warangalone is administered systemically. TPA-induced ear edema is induced by topical application of TPA to the mouse ear, and Warangalone is administered locally. The reduction in edema is measured as an indicator of anti-inflammatory activity.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for Warangalone are not provided in the available sources. The compound has a molecular weight of 404.47 and a molecular formula of C25H24O5. It is soluble in DMSO. It is typically stored as a solid powder at -20°C for up to 1 year. Stock solutions can be stored at 0-4°C for up to 1 month.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Warangalone are not provided in the available sources. As a research compound, it is intended for laboratory use only and is not approved for human therapeutic applications. The compound is a natural product with anti-malarial, anti-inflammatory, and cytotoxic activities. Standard safety precautions should be followed when handling this compound.
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| References |
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| Additional Infomation |
Warangalone has reportedly been found in Maclura pomifera, Euchresta horsfieldii, and other organisms with available data.
Warangalone is an anti-malarial compound which can inhibit the growth of both strains of parasite 3D7 (chloroquine sensitive) and K1 (chloroquine resistant) with IC50s of 4.8 μg/mL and 3.7 μg/mL, respectively. It also inhibits protein kinase A with an IC50 of 3.5 μM. It shows anti-inflammatory activity on PLA2-induced paw edema and TPA-induced ear edema in mice. It induces apoptosis in HL-60 cells. |
| Molecular Formula |
C25H24O5
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|---|---|
| Molecular Weight |
404.45506
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| Exact Mass |
404.162
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| Elemental Analysis |
C, 74.24; H, 5.98; O, 19.78
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| CAS # |
4449-55-2
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| Related CAS # |
2934.99.03.00
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| PubChem CID |
5379679
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
627.0±55.0 °C at 760 mmHg
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| Flash Point |
216.7±25.0 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.628
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| LogP |
7.87
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
752
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1C(C(O)=C(C=CC(C)(C)O2)C2=C3C/C=C(C)\C)=C3OC=C1C4=CC=C(O)C=C4
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| InChi Key |
HGHOPAZIUPORIN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H24O5/c1-14(2)5-10-18-23-17(11-12-25(3,4)30-23)21(27)20-22(28)19(13-29-24(18)20)15-6-8-16(26)9-7-15/h5-9,11-13,26-27H,10H2,1-4H3
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| Chemical Name |
5-hydroxy-7-(4-hydroxyphenyl)-2,2-dimethyl-10-(3-methylbut-2-en-1-yl)-2H,6H-pyrano[3,2-g]chromen-6-one
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| Synonyms |
Warangalone; Scandenolone
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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) |
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 | 2.4724 mL | 12.3622 mL | 24.7243 mL | |
| 5 mM | 0.4945 mL | 2.4724 mL | 4.9449 mL | |
| 10 mM | 0.2472 mL | 1.2362 mL | 2.4724 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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