| 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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| Targets |
Febrifugine dihydrochloride, like its parent compound febrifugine, exhibits antimalarial activity against Plasmodium species. Its exact molecular target is not fully elucidated, but it is believed to inhibit protein synthesis in the malaria parasite. The compound also shows potential therapeutic activity regarding cancer, fibrosis, and inflammatory diseases. As a quinazolinone alkaloid, it serves as a lead scaffold for antimalarial drug discovery.
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| ln Vitro |
Febrifugine dihydrochloride demonstrates in vitro antimalarial activity against Plasmodium falciparum. The compound's activity can be assessed in parasite cultures by measuring growth inhibition. Its cytotoxicity and selectivity can be evaluated in mammalian cell lines. The compound's biological activity has been characterized in various in vitro assays, supporting its potential as an antimalarial agent and its utility as a lead compound for medicinal chemistry optimization.
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| ln Vivo |
Febrifugine dihydrochloride has been studied in vivo for its antimalarial and other therapeutic activities. As a salt form of febrifugine, it is expected to have improved aqueous solubility and bioavailability compared to the free base. The compound has been evaluated in animal models of malaria, where it reduces parasitemia and mortality. Its therapeutic potential in cancer, fibrosis, and inflammatory diseases has also been investigated in preclinical models.
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| Enzyme Assay |
Non-cellular enzyme assays for febrifugine dihydrochloride are limited as its precise molecular target is not fully characterized. The compound's antimalarial activity can be assessed in cell-free systems by measuring its effect on parasite protein synthesis or other biochemical processes. Its interaction with potential molecular targets can be studied using affinity chromatography or surface plasmon resonance (SPR) approaches. The compound's physicochemical properties, including solubility and stability, can be characterized using standard analytical techniques.
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| Cell Assay |
In vitro cellular assays for febrifugine dihydrochloride involve treating Plasmodium falciparum cultures with the compound and assessing parasite growth inhibition. Cultures are incubated with varying concentrations of the compound for 48-72 hours, and parasite viability is measured using a [³H]-hypoxanthine incorporation assay or by microscopy to count parasitemia. IC50 values are determined from dose-response curves. Cytotoxicity is assessed in mammalian cell lines using MTT or CellTiter-Glo® assays.
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| Animal Protocol |
In vivo animal experiments with febrifugine dihydrochloride are conducted in murine malaria models. Mice infected with Plasmodium are treated with the compound via oral or intraperitoneal administration. Parasitemia is monitored by blood smears, and survival rates are recorded. The compound's efficacy and toxicity are assessed, and its pharmacokinetic properties are characterized. Studies in models of cancer, fibrosis, and inflammatory diseases have also been conducted to evaluate its broader therapeutic potential.
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| ADME/Pharmacokinetics |
Febrifugine dihydrochloride has a molecular weight of 374.26 and a molecular formula of C16H21Cl2N3O3. It is a white to off-white solid at room temperature. The compound is soluble in water (15 mg/mL) and is typically stored as a powder at -20°C for up to 3 years or at 4°C for 2 years. Purity is typically ≥98%. The compound is stable under recommended storage conditions and is protected from light and moisture.
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| Toxicity/Toxicokinetics |
Febrifugine dihydrochloride is a research compound for laboratory use only and is not intended for human therapeutic or diagnostic use. As a salt form of febrifugine, it retains the hepatotoxicity and emetic side effects associated with the parent compound. Standard laboratory safety precautions should be followed when handling the compound, as it may cause skin, eye, and respiratory irritation. The compound should be handled in a well-ventilated area with appropriate personal protective equipment.
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| References |
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| Additional Infomation |
See also: Pildralazine dihydrochloride (note moved to).
Febrifugine dihydrochloride (CAS 32434-42-7) is the dihydrochloride salt form of the quinazolinone alkaloid febrifugine, which is extracted from Dichroa febrifuga. It exhibits antimalarial activity and has been studied for potential therapeutic applications in malaria, cancer, fibrosis, and inflammatory diseases. The compound's improved aqueous solubility compared to the free base makes it a valuable tool for research applications. It is available from various commercial suppliers for research use only. |
| Molecular Formula |
C16H19N3O3.2[HCL]
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|---|---|
| Molecular Weight |
374.26224
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| Exact Mass |
373.096
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| CAS # |
32434-42-7
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| Related CAS # |
Febrifugine;24159-07-7
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| PubChem CID |
25112190
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| Appearance |
White to off-white solid powder
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| Melting Point |
220-222 °C (decomp)
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| Source |
Originated from plants: Saxifragaceae Dichroa febrifuga Lour
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| LogP |
2.401
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
466
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1C[C@@H]([C@H](NC1)CC(=O)CN2C=NC3=CC=CC=C3C2=O)O.Cl.Cl
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| InChi Key |
RDUHYEILHQUTIR-AMTWEWDESA-N
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| InChi Code |
InChI=1S/C16H19N3O3.2ClH/c20-11(8-14-15(21)6-3-7-17-14)9-19-10-18-13-5-2-1-4-12(13)16(19)22;;/h1-2,4-5,10,14-15,17,21H,3,6-9H2;2*1H/t14-,15+;;/m1../s1
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| Chemical Name |
3-[3-[(2R,3S)-3-hydroxypiperidin-2-yl]-2-oxopropyl]quinazolin-4-one;dihydrochloride
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| Synonyms |
ISF-2123, Febrifugine dihydrochloride, (+)-Febrifugine dihydrochloride, Atensil
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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: ~8.3 mg/mL (~22.3 mM; with ultrasonication and warming by heating to 60°C)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.62 mg/mL (1.66 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 (6.2 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: ≥ 0.62 mg/mL (1.66 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 (6.2 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: ≥ 0.62 mg/mL (1.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 (6.2 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 | 2.6719 mL | 13.3597 mL | 26.7194 mL | |
| 5 mM | 0.5344 mL | 2.6719 mL | 5.3439 mL | |
| 10 mM | 0.2672 mL | 1.3360 mL | 2.6719 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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