フシジン酸
Based on 2 publication(s) in Google Scholar
Fusidic acid (Fusidate) a bacteriostatic antibiotic produced from the Fusidium coccineum fungus, belongs to the class of steroids. Fusidic acid has no corticosteroid effects. Fusidic acid inhibits the growth of bacteria by preventing the release of translation elongation factor G (EF-G) from the ribosome. Fusidic acid holds promise for research in anticancer and anti-infective applications..
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.79%
- CAS 番号: 6990-06-3
- 分子式: C31H48O6
- 分子量:516.71
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
MedChemExpress(MCE)の使用を引用している文献 Fusidic acid
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
>194 μM
Compound: 1
|
Cytotoxicity against CHO assessed as cell viability after 48 hrs by MTT assay
Cytotoxicity against CHO assessed as cell viability after 48 hrs by MTT assay
|
10.1039/C5MD00343A |
| CHO | IC50 |
>194 μM
Compound: Fusidic acid
|
Cytotoxicity against CHO cells
Cytotoxicity against CHO cells
|
[PMID: 28012840] |
| CHO | IC50 |
194 μM
Compound: 1
|
Cytotoxicity against CHO cells by MTT assay
Cytotoxicity against CHO cells by MTT assay
|
[PMID: 30108825] |
| CHO-K1 | IC50 |
>194 μM
Compound: 1
|
Cytotoxicity against CHOK1 cells assessed as reduction in cell viability
Cytotoxicity against CHOK1 cells assessed as reduction in cell viability
|
[PMID: 32362386] |
| HEK293 | CC50 |
>32 μg/mL
Compound: FA
|
Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 72 hrs by MTT assay
|
[PMID: 30445262] |
| HeLa | IC50 |
>100 μM
Compound: FA
|
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 72 hrs by MTT assay
|
[PMID: 30445262] |
| MKN-45 | IC50 |
>100 μM
Compound: FA
|
Cytotoxicity against human MKN45 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human MKN45 cells assessed as reduction in cell viability after 72 hrs by MTT assay
|
[PMID: 30445262] |
| RAW264.7 | IC50 |
61.26 μM
Compound: FA
|
Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay
Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay
|
[PMID: 37544187] |
| Sf21 | IC50 |
11.5 μM
Compound: Fusidic acid
|
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
|
[PMID: 21965623] |
| Sf21 | IC50 |
17.4 μM
Compound: Fusidic acid
|
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
|
[PMID: 21965623] |
| U-87MG ATCC | IC50 |
>100 μM
Compound: FA
|
Cytotoxicity against human U87 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human U87 cells assessed as reduction in cell viability after 72 hrs by MTT assay
|
[PMID: 30445262] |
| Vero | IC50 |
105.8 μg/mL
Compound: Fusidic acid
|
Cytotoxicity against african green monkey Vero cells after 72 hrs
Cytotoxicity against african green monkey Vero cells after 72 hrs
|
[PMID: 8988597] |
Fusidic acid (100-200 μM, 72 h) primarily inhibits the proliferation of breast cancer (MCF-7, MDA-MB-231), thyroid cancer (8505C, TPC1), and cervical cancer (Caski, HeLa) cells through cell cycle arrest rather than apoptosis[3]. Fusidic acid (0.01-100 × MIC, 24 h) exhibits stable intracellular antibacterial activity against methicillin-sensitive Staphylococcus aureus and methicillin-resistant Staphylococcus aureus in THP-1 cells, with potency comparable to Clindamycin (HY-B1455) and Linezolid (HY-10394). MIC at pH 7.4 was 0.25 mg/L, whereas MIC at pH 5.5 decreased to 0.01 mg/L[4]. Fusidic acid (125 mg/L, 30 min) demonstrates enhanced antibacterial activity against methicillin-sensitive Staphylococcus aureus and significantly increased intracellular accumulation under acidic conditions (pH 5.5)[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7, MDA-MB-231 (breast cancer); 8505C, TPC1 (thyroid cancer); Caski, HeLa (cervical cancer)
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Concentration:10 μM, 100 μM, 200 μM
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Incubation Time:72 hours
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Result:Inhibited cell proliferation in a dose-dependent manner: Breast cancer cells (MCF-7: 100 μM, 28%; MDA-MB-231: 100 μM, 32%) Thyroid cancer cells (8505C: 200 μM, 43%; TPC1: 100 μM, 45%) Cervical cancer cells (Caski: 200 μM, 29%; HeLa: 200 μM, 38%)
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Cell Line:MCF-7, MDA-MB-231 (breast cancer); 8505C, TPC1 (thyroid cancer); Caski, HeLa (cervical cancer)
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Concentration:100 μM, 200 μM
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Incubation Time:72 hours
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Result:Induced different phases of cell cycle arrest depending on cell type: Breast cancer (MCF-7, MDA-MB-231): G0/G1 phase arrest (MCF-7: 200 μM, 42%; MDA-MB-231: 200 μM, 16%). Thyroid cancer (8505C, TPC1): S phase arrest (8505C: 200 μM, 12%; TPC1: 200 μM, 7%). Cervical cancer: Caski: G0/G1 increase 11%; HeLa: G2/M increase 15%.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cyclophosphamide (HY-17420)-induced immunosuppressed vaginal candidiasis Balb/c mouse model[5]
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Dosage:1 mg/mL
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Administration:Vaginal gel application (VGA), 20 μL per mouse, once daily for 5 days
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Result:Significantly reduced Candida albicans CFU in vaginal lavage and fungal burden in vaginal tissue. Caused that antifungal activity was further enhanced when combined with Fluconazole (HY-B0101). Led to less vaginal tissue damage and inflammation compared to control.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 6990-06-3
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性状 Solid
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分子量 516.71
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分子式 C31H48O6
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Color White to off-white
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SMILES
C[C@@H]([C@]1([H])CC[C@]([C@@](C[C@@H]/2OC(C)=O)3C)4C)[C@H](O)CC[C@]1(C)[C@]4([H])[C@H](O)C[C@@]3([H])C2=C(C(O)=O)/CC/C=C(C)\C
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別名
Fusidic acid; Fusidate; SQ-16603
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Structure Classification
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Initial Source
Fusidium
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (2)
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Journal Impact Factor
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Most Recent
溶剤 & 溶解度
DMSO : 100 mg/mL (193.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (285 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Curbete MM, et al. A Critical Review of the Properties of Fusidic Acid and Analytical Methods for Its Determination. Crit Rev Anal Chem. 2016;46(4):352-360. [Content Brief]
[2]. Payne AJ, et al. Fusidic acid is an effective treatment against Toxoplasma gondii and Listeria monocytogenes in vitro, but not in mice. Parasitol Res. 2013;112(11):3859-3863. [Content Brief]
[3]. Kim JY, et al. Growth inhibition by fusidic acid in cervical, thyroid, and breast carcinoma cell lines. Obstet Gynecol Sci. 2023 Mar;66(2):100-106. [Content Brief]
[4]. Lemaire S, et al. Activity of fusidic acid against extracellular and intracellular Staphylococcus aureus: influence of pH and comparison with linezolid and clindamycin. Clin Infect Dis. 2011 Jun;52 Suppl 7:S493-503. [Content Brief]
[5]. Gomaa SE, et al. The anti-staphylococcal fusidic acid as an efflux pump inhibitor combined with fluconazole against vaginal candidiasis in mouse model. BMC Microbiol. 2024 Feb 10;24(1):54. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9353 mL | 9.6766 mL | 19.3532 mL | 48.3830 mL |
| 5 mM | 0.3871 mL | 1.9353 mL | 3.8706 mL | 9.6766 mL | |
| 10 mM | 0.1935 mL | 0.9677 mL | 1.9353 mL | 4.8383 mL | |
| 15 mM | 0.1290 mL | 0.6451 mL | 1.2902 mL | 3.2255 mL | |
| 20 mM | 0.0968 mL | 0.4838 mL | 0.9677 mL | 2.4192 mL | |
| 25 mM | 0.0774 mL | 0.3871 mL | 0.7741 mL | 1.9353 mL | |
| 30 mM | 0.0645 mL | 0.3226 mL | 0.6451 mL | 1.6128 mL | |
| 40 mM | 0.0484 mL | 0.2419 mL | 0.4838 mL | 1.2096 mL | |
| 50 mM | 0.0387 mL | 0.1935 mL | 0.3871 mL | 0.9677 mL | |
| 60 mM | 0.0323 mL | 0.1613 mL | 0.3226 mL | 0.8064 mL | |
| 80 mM | 0.0242 mL | 0.1210 mL | 0.2419 mL | 0.6048 mL | |
| 100 mM | 0.0194 mL | 0.0968 mL | 0.1935 mL | 0.4838 mL |