| Size | Price | Stock | Qty |
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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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| Other Sizes |
Purity: ≥98%
| Targets |
Filastatin targets key virulence factors in pathogenic Candida species, including adhesion and filamentation. It inhibits adhesion by multiple pathogenic Candida species with an IC50 of ~3 µM in a GFP-based adhesion assay. Filastatin inhibits the yeast-to-hyphal morphological transition and the induction of the hyphal-specific HWP1 promoter. By inhibiting these virulence factors, Filastatin prevents Candida from adhering to surfaces and forming biofilms, and it blocks the transition to the invasive hyphal form. The compound is non-toxic to human cells, making it a promising candidate for the treatment of Candida infections.
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| ln Vitro |
In vitro studies have demonstrated that Filastatin is a long-lasting inhibitor of Candida albicans filamentation. It inhibits adhesion by multiple pathogenic Candida species with an IC50 of ~3 µM in a GFP-based adhesion assay. Filastatin inhibits the yeast-to-hyphal morphological transition and the induction of the hyphal-specific HWP1 promoter. It blocks the ability of Candida albicans and other Candida species to bind to polystyrene and human cells. These in vitro findings confirm the compound's mechanism of action as an inhibitor of Candida virulence factors. Filastatin is non-toxic to human cells, making it a promising antifungal agent.
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| ln Vivo |
In vivo studies on Filastatin are limited, but the compound has demonstrated antifungal activity in preclinical models. As an inhibitor of Candida adhesion and filamentation, Filastatin has the potential to prevent and treat Candida infections in vivo. However, specific in vivo data for Filastatin, including efficacy in animal models of candidiasis and pharmacokinetic parameters, are not extensively documented in publicly available sources. The compound's non-toxicity to human cells suggests a favorable safety profile. Filastatin is primarily used as a research tool for studying Candida virulence and for developing new antifungal therapies.
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| Enzyme Assay |
Non-cellular assays for Filastatin typically involve measuring its ability to inhibit Candida adhesion to surfaces, such as polystyrene or human cells. These assays use Candida cells and a fluorescent or colorimetric readout to quantify adhesion. Filastatin is tested at various concentrations to determine its IC50 for inhibiting adhesion. Alternatively, assays measuring the inhibition of the yeast-to-hyphal transition can be performed by culturing Candida in hyphal-inducing conditions and assessing the percentage of hyphal cells microscopically. The inhibition of the HWP1 promoter can be assessed using reporter assays. These assays are essential for characterizing the mechanism of action and potency of Filastatin as an inhibitor of Candida virulence factors.
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| Cell Assay |
In vitro cell-based assays for Filastatin typically use Candida species, such as Candida albicans, and human cell lines to assess the compound's effects on adhesion and filamentation. Candida cells are cultured in appropriate media and treated with Filastatin at various concentrations. Adhesion to polystyrene or to human cell monolayers is assessed using fluorescent or colorimetric assays. Filamentation is induced using appropriate conditions (e.g., serum, temperature), and the percentage of hyphal cells is assessed microscopically. Cytotoxicity to human cells is assessed using MTT or similar assays to confirm the compound's non-toxicity. Filastatin is typically dissolved in DMSO and diluted in culture medium, with DMSO controls included to account for solvent effects.
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| Animal Protocol |
In vivo animal studies for Filastatin would typically involve mouse models of candidiasis, such as disseminated candidiasis or oral/vaginal candidiasis models. Animals would be infected with Candida albicans and treated with Filastatin at various doses, typically administered orally or intravenously. Fungal burden in tissues, survival, and clinical signs would be assessed. However, specific published in vivo data for Filastatin are not extensively documented. The compound is primarily used as a research tool for studying Candida virulence and for developing new antifungal therapies. Further studies are needed to validate its in vivo efficacy.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Filastatin are limited in publicly available sources. The compound has a molecular weight of 359.81 g/mol and a molecular formula of C18H18ClN3O3. As a small molecule, Filastatin is expected to be absorbed and distributed to tissues. However, detailed PK parameters such as half-life, Cmax, AUC, and bioavailability have not been extensively reported. The compound's solubility and stability are important factors for its use in in vitro and in vivo studies. Research-grade Filastatin is intended for laboratory use only. Further pharmacokinetic studies are needed to fully characterize the compound's absorption, distribution, metabolism, and excretion.
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| Toxicity/Toxicokinetics |
Toxicological data for Filastatin indicate that the compound is non-toxic to human cells. As a research compound, Filastatin is intended for laboratory use only and is not for human consumption. Standard toxicological assessments, including acute and chronic toxicity studies, would be required for clinical development. However, these data are not publicly available. The compound's non-toxicity to human cells suggests a favorable safety profile. As with all research chemicals, appropriate safety precautions should be taken when handling Filastatin.
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| References | |
| Additional Infomation |
Filastatin is a cell-permeable, non-toxic small-molecule inhibitor of Candida adhesion and filamentation. It has the CAS number 431996-53-1. Filastatin inhibits adhesion with an IC50 of ~3 µM and blocks the yeast-to-hyphal transition. It is non-toxic to human cells. Filastatin is not approved for clinical use and is strictly a research compound for studying Candida virulence and antifungal drug development.
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| Molecular Formula |
C18H18CLN3O3
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|---|---|
| Molecular Weight |
359.81
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| Exact Mass |
359.104
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| Elemental Analysis |
C, 60.09; H, 5.04; Cl, 9.85; N, 11.68; O, 13.34
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| CAS # |
431996-53-1
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| PubChem CID |
2911546
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| Appearance |
Solid powder
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| LogP |
4.045
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
482
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=C(C)C=CC(=C1)C(N1CCN(C2C=CC(=CC=2)[N+](=O)[O-])CC1)=O
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| InChi Key |
PNECWWUOUHGWQG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H18ClN3O3/c1-13-2-3-14(12-17(13)19)18(23)21-10-8-20(9-11-21)15-4-6-16(7-5-15)22(24)25/h2-7,12H,8-11H2,1H3
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| Chemical Name |
(3-Chloro-4-methyl-phenyl)-[4-(4-nitro-phenyl)-piperazin-1-yl]-methanone
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| Synonyms |
Filastatin;
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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 (~347.4 mM; with ultrasonication)
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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 | 2.7792 mL | 13.8962 mL | 27.7924 mL | |
| 5 mM | 0.5558 mL | 2.7792 mL | 5.5585 mL | |
| 10 mM | 0.2779 mL | 1.3896 mL | 2.7792 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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