Febrifugine

CAS# 24159-07-7

Febrifugine

Catalog No. BCN3269----Order now to get a substantial discount!

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Quality Control of Febrifugine

Number of papers citing our products

Chemical structure

Febrifugine

3D structure

Chemical Properties of Febrifugine

Cas No. 24159-07-7 SDF Download SDF
PubChem ID 63224 Appearance Powder
Formula C16H19N3O3 M.Wt 301.3
Type of Compound Alkaloids Storage Desiccate at -20°C
Solubility Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc.
Chemical Name 3-[3-[(2S,3R)-3-hydroxypiperidin-2-yl]-2-oxopropyl]quinazolin-4-one
SMILES C1CC(C(NC1)CC(=O)CN2C=NC3=CC=CC=C3C2=O)O
Standard InChIKey FWVHWDSCPKXMDB-LSDHHAIUSA-N
Standard InChI InChI=1S/C16H19N3O3/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/t14-,15+/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Source of Febrifugine

The roots of Dichroa febrifuga

Biological Activity of Febrifugine

DescriptionFebrifugine is an effective coccidiostat, possesses schizonticide props; it and its derivatives shows high degree of antimalarial activity but use limited by toxicity .
TargetsAntifection | PfcPRS | IL Receptor | IFN-γ
In vivo

The cytoplasmic prolyl-tRNA synthetase of the malaria parasite is a dual-stage target of febrifugine and its analogs.[Pubmed: 25995223]

Sci Transl Med. 2015 May 20;7(288):288ra77.

The emergence of drug resistance is a major limitation of current antimalarials. The discovery of new druggable targets and pathways including those that are critical for multiple life cycle stages of the malaria parasite is a major goal for developing next-generation antimalarial drugs.
METHODS AND RESULTS:
Using an integrated chemogenomics approach that combined drug resistance selection, whole-genome sequencing, and an orthogonal yeast model, we demonstrate that the cytoplasmic prolyl-tRNA (transfer RNA) synthetase (PfcPRS) of the malaria parasite Plasmodium falciparum is a biochemical and functional target of Febrifugine and its synthetic derivative halofuginone. Febrifugine is the active principle of a traditional Chinese herbal remedy for malaria. We show that treatment with Febrifugine derivatives activated the amino acid starvation response in both P. falciparum and a transgenic yeast strain expressing PfcPRS. We further demonstrate in the Plasmodium berghei mouse model of malaria that halofuginol, a new halofuginone analog that we developed, is active against both liver and asexual blood stages of the malaria parasite.
CONCLUSIONS:
Halofuginol, unlike halofuginone and Febrifugine, is well tolerated at efficacious doses and represents a promising lead for the development of dual-stage next-generation antimalarials.

Possible involvement of IFN-gamma in early mortality of Plasmodium berghei NK65-infected BALB/c mice after febrifugine treatment.[Pubmed: 19062681]

Southeast Asian J Trop Med Public Health. 2008 Nov;39(6):949-58.


METHODS AND RESULTS:
Parasitemia patterns, survival and cytokine levels of Plasmodium berghei NK65-infected BALB/c mice, treated orally with the alkaloidal mixture of Febrifugine and isoFebrifugine at a dose of 1 mg/kg twice a day for 4 consecutive days were monitored. Whereas the untreated mice showed a progressive increase in parasitemia and ultimate death, the alkaloid mixture-treated group showed a transient suppression of parasitemia during the course of treatment. However, the parasitemia increased on discontinuation of treatment, leading to earlier death of mice in the treated group than in the infected but untreated controls. Mice in the infected but untreated group displayed a significant elevation in serum IFN-gammay levels during the first week post-infection (pI) and from Day 14 pI, relative to the levels in the uninfected controls. In contrast, although mice in the alkaloid mixture-treated group displayed no significant elevation in serum IFN-gamma levels during the first week pI, they showed considerable levels on Day 14 pI. There were no significant differences in serum IL-4 levels among the groups. The titers of the parasite-specific IgG1, IgG2a, IgG2b and IgG3 were significantly elevated from Day 11 pI in both the treated and untreated groups. There was a significant difference in survival duration between the IFN-gamma-/- mutant and BALB/c mice. IFN-gamma-/- mutant mice showed a decrease in parasitemia levels while receiving medication, which was significantly lower than those of the treated BALB/c mice.
CONCLUSIONS:
The results of the present study suggest that although IFN-gamma is significant for protective immunity in mice with malaria infection, it may play an adverse role post-medication, causing earlier mortality of treated BALB/c mice.

Protocol of Febrifugine

Structure Identification
J Adv Pharm Technol Res. 2013 Jan;4(1):50-60.

Pharmacophore modeling and 3D quantitative structure-activity relationship analysis of febrifugine analogues as potent antimalarial agent.[Pubmed: 23662282]

Febrifugine and its derivatives are effective against Plasmodium falciparum.
METHODS AND RESULTS:
Using PHASE algorithm, a five-point pharmacophore model with two hydrogen bond acceptor (A), one positively ionizable (P) and two aromatic rings (R), was developed to derive a predictive ligand-based statistically significant 3D-quantitative structure-activity relationship (QSAR) model (r(2) = 0.972, SD = 0.3, F = 173.4, Q(2) = 0.712, RMSE = 0.3, Person-R = 0.94, and r(2) pred = 0.8) to explicate the structural attributes crucial for antimalarial activity.
CONCLUSIONS:
The developed pharmacophore model and 3D QSAR model can be a substantial tool for virtual screening and related antimalarial drug discovery research.

Febrifugine Dilution Calculator

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Febrifugine Molarity Calculator

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Preparing Stock Solutions of Febrifugine

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.319 mL 16.5948 mL 33.1895 mL 66.379 mL 82.9738 mL
5 mM 0.6638 mL 3.319 mL 6.6379 mL 13.2758 mL 16.5948 mL
10 mM 0.3319 mL 1.6595 mL 3.319 mL 6.6379 mL 8.2974 mL
50 mM 0.0664 mL 0.3319 mL 0.6638 mL 1.3276 mL 1.6595 mL
100 mM 0.0332 mL 0.1659 mL 0.3319 mL 0.6638 mL 0.8297 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on Febrifugine

Possible involvement of IFN-gamma in early mortality of Plasmodium berghei NK65-infected BALB/c mice after febrifugine treatment.[Pubmed:19062681]

Southeast Asian J Trop Med Public Health. 2008 Nov;39(6):949-58.

Parasitemia patterns, survival and cytokine levels of Plasmodium berghei NK65-infected BALB/c mice, treated orally with the alkaloidal mixture of Febrifugine and isoFebrifugine at a dose of 1 mg/kg twice a day for 4 consecutive days were monitored. Whereas the untreated mice showed a progressive increase in parasitemia and ultimate death, the alkaloid mixture-treated group showed a transient suppression of parasitemia during the course of treatment. However, the parasitemia increased on discontinuation of treatment, leading to earlier death of mice in the treated group than in the infected but untreated controls. Mice in the infected but untreated group displayed a significant elevation in serum IFN-gammay levels during the first week post-infection (pI) and from Day 14 pI, relative to the levels in the uninfected controls. In contrast, although mice in the alkaloid mixture-treated group displayed no significant elevation in serum IFN-gamma levels during the first week pI, they showed considerable levels on Day 14 pI. There were no significant differences in serum IL-4 levels among the groups. The titers of the parasite-specific IgG1, IgG2a, IgG2b and IgG3 were significantly elevated from Day 11 pI in both the treated and untreated groups. There was a significant difference in survival duration between the IFN-gamma-/- mutant and BALB/c mice. IFN-gamma-/- mutant mice showed a decrease in parasitemia levels while receiving medication, which was significantly lower than those of the treated BALB/c mice. The results of the present study suggest that although IFN-gamma is significant for protective immunity in mice with malaria infection, it may play an adverse role post-medication, causing earlier mortality of treated BALB/c mice.

The cytoplasmic prolyl-tRNA synthetase of the malaria parasite is a dual-stage target of febrifugine and its analogs.[Pubmed:25995223]

Sci Transl Med. 2015 May 20;7(288):288ra77.

The emergence of drug resistance is a major limitation of current antimalarials. The discovery of new druggable targets and pathways including those that are critical for multiple life cycle stages of the malaria parasite is a major goal for developing next-generation antimalarial drugs. Using an integrated chemogenomics approach that combined drug resistance selection, whole-genome sequencing, and an orthogonal yeast model, we demonstrate that the cytoplasmic prolyl-tRNA (transfer RNA) synthetase (PfcPRS) of the malaria parasite Plasmodium falciparum is a biochemical and functional target of Febrifugine and its synthetic derivative halofuginone. Febrifugine is the active principle of a traditional Chinese herbal remedy for malaria. We show that treatment with Febrifugine derivatives activated the amino acid starvation response in both P. falciparum and a transgenic yeast strain expressing PfcPRS. We further demonstrate in the Plasmodium berghei mouse model of malaria that halofuginol, a new halofuginone analog that we developed, is active against both liver and asexual blood stages of the malaria parasite. Halofuginol, unlike halofuginone and Febrifugine, is well tolerated at efficacious doses and represents a promising lead for the development of dual-stage next-generation antimalarials.

Pharmacophore modeling and 3D quantitative structure-activity relationship analysis of febrifugine analogues as potent antimalarial agent.[Pubmed:23662282]

J Adv Pharm Technol Res. 2013 Jan;4(1):50-60.

Febrifugine and its derivatives are effective against Plasmodium falciparum. Using PHASE algorithm, a five-point pharmacophore model with two hydrogen bond acceptor (A), one positively ionizable (P) and two aromatic rings (R), was developed to derive a predictive ligand-based statistically significant 3D-quantitative structure-activity relationship (QSAR) model (r(2) = 0.972, SD = 0.3, F = 173.4, Q(2) = 0.712, RMSE = 0.3, Person-R = 0.94, and r(2) pred = 0.8) to explicate the structural attributes crucial for antimalarial activity. The developed pharmacophore model and 3D QSAR model can be a substantial tool for virtual screening and related antimalarial drug discovery research.

Description

Febrifugine is a quinazolinone alkaloid found in the roots and leaves of Dichroa febrifuga, with antimalarial activity .

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