| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: =99.62%
Micafungin Sodium (also known as FK463; Mycamine sodium), an echinocandin antifungal agent, is a novel and potent inhibitor of 1, 3-beta-D-glucan synthesis, which is used as an antifungal drug. Micafungin as an antifungal agent is known to inhibit 1,3-β-D-glucan synthesis in Candida albicans. In 13 out of 18 P. Aeruginosa isolates tested, micafungin significantly reduced biofilm biomass. In all 9 P. Aeruginosa isolates tested, micafungin decreased the expression of ndvB, which encoded the cell wall 1,3-β-D-glucan. Also, it decreased the expression of biofilm encoding genes for alginate and pellicles (algC and pelC, respectively).
| Targets |
Antifungal agent; 1, 3-beta-D-glucan synthesis
|
|---|---|
| ln Vitro |
The majority of the isolates exhibit phenotypic reductions in biofilm formation when exposed to 10 mg/mL micafungin. In comparison to their untreated counterparts, the levels of mRNA transcription for every gene examined are likewise markedly lower in samples treated with micafungin[1]. KB425796-C and micafungin together exhibit fungicidal effects that significantly lower CFU counts, as opposed to fungistatic effects that show no CFU reduction at any of the time points under investigation[2].
|
| ln Vivo |
When mice are given micafungin (1 mg/kg) instead of saline, their survival is significantly extended. When KB425796-C (32 mg/kg) and micafungin (0.1 mg/kg) are administered together, animals exhibit a tendency for longer survival than when micafungin (0.1 mg/kg) is administered alone. Mice treated with micafungin show a decrease in the number of CFUs in their livers, albeit with a smaller clearance effect than in their kidneys. When micafungin and KB425796-C are used in combination, the number of CFUs is significantly lower than when micafungin is used alone at all doses that were studied. When combined with micafungin, KB425796-C has a higher clearance effect than when it is administered to animals with AMPH.
|
| Enzyme Assay |
This study assesses the potential effect of micafungin, an antifungal agent known to inhibit 1,3-β-D-glucan synthesis in Candida albicans, on biofilm formation of selected Pseudomonas aeruginosa isolates by decreasing the synthesis of extracellular matrix β-D-glucan forming units. The effect of an optimal therapeutic dose of 10 mg ml(-1) micafungin on the production of biofilm was monitored in vitro using a microtiter plate assay. Phenotypic reduction in the formation of biofilm was significant (based on average optical density; p < 0.05) in most of the isolates. Moreover, the relative gene expression of biofilm encoding genes for alginate and pellicles (algC and pelC, respectively), and the cell wall 1,3-β-D-glucan encoding gene (ndvB) was evaluated using quantitative reverse transcription PCR. For all the genes tested, the levels of mRNA transcription were also decreased significantly (p < 0.05) in micafungin-treated samples cf. their untreated counterparts. In conclusion, this study presents micafungin as a potential agent for disrupting the structure of a biofilm of P. aeruginosa allowing the possible exposure and treatment of core-planktonic cells[1].
|
| Cell Assay |
Every fungal isolate is statically cultured for 24 hours at 30°C in yeast-maltose (YM) agar broth. In YM broth medium, Cryptococcus neoformans YC203 is cultivated for 20 hours at 30°C and 200 r.p.m. shaking. Washing the cultured cells once with sterile saline yields a cell suspension. Spores from A. fumigatus FP1305 are harvested in sterile saline and collected by filtering through gauze after the strainer is cultivated on a potato dextrose agar (PDA) slant for four days.The antifungal activity of RPMI 1640 medium supplemented with l-glutamine (without sodium bicarbonate) and buffered to pH 7.0 with 0.165 m MOPS is measured in 96-well culture plates using the micro-broth dilution method against all isolates, except for C. neoformans. YNBD (yeast nitrogen base-glucose) medium is used for C. neoformans. In the assay, 1×105 CFU/well of the test microorganism is inoculated into each well, and the plates are then incubated at 37°C for 20 or 48 hours. Microscopic observation establishes two end points: MEC, which is defined as a significant decrease in fungal growth, and MIC, which is defined as a total inhibition of growth.
|
| Animal Protocol |
2.0×106 A. fumigatus FP1305 spores are intravenously injected into eight groups of ten female DBA/2 mice (7 weeks old). The following therapies are administered to the test groups: AMPH is administered intraperitoneally (i.p.) once daily (q.d.); micafungin is administered subcutaneously (s.c.) at doses of 0.1, 0.32, or 1 mg/kg of body weight (q.d.); micafungin is administered s.c. at doses of 0.1, 0.32, or 1 mg/kg q.d.; in addition, KB425796-C is administered i.p. at doses of 32 mg/kg twice daily (b.i.d.); and saline is administered (b.i.d.). On days one and two, medications are given. After the treatment is over, five mice per group are killed one day later. Following their aseptic removal, the kidneys and livers are homogenized in 5 milliliters of sterile saline. The homogenates are serially diluted 10-fold, plated on PDA, and then incubated for 48 hours at 37°C. The resulting number of CFU per gram of tissue is then computed. For thirty-one days following the challenge, the survival rate of the five mice from each group that remain are monitored every day.
|
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation No information is available on the use of micafungin during breastfeeding. Because micafungin is >99% bound to plasma proteins and has poor oral bioavailability, it is unlikely to reach the milk and be absorbed by the infant. Micafungin can safely be given intravenously to infants under 4 months of age. Any amount absorbed from milk is likely to be far less than an infant dose. If micafungin is required by the mother, it is not a reason to discontinue breastfeeding. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References |
|
| Additional Infomation |
Micafungin sodium is an organic sodium salt and an antibiotic antifungal drug.
Micafungin Sodium is the sodium salt form of micafungin, a semi-synthetic echinocandin derived from a natural product of the fungus Coleophoma empetri with antifungal activity. Micafungin, like other cyclic lipopeptides, noncompetitively inhibits the fungal specific enzyme 1,3-beta-D-glucan synthase, an enzyme essential for the synthesis of the important fungal cell wall component 1,3-beta-D-glucan. By preventing the synthesis of 1,3-beta-D-glucan, the cell wall is weakened which leads to osmotic lysis and eventually fungal cell death. A cyclic lipo-hexapeptide echinocandin antifungal agent that is used for the treatment and prevention of CANDIDIASIS. See also: Micafungin (has active moiety). Drug Indication Mycamine is indicated for: Adults, adolescents ⥠16 years of age and elderlytreatment of invasive candidiasis; treatment of oesophageal candidiasis in patients for whom intravenous therapy is appropriate; prophylaxis of Candida infection in patients undergoing allogeneic haematopoietic stem-cell transplantation or patients who are expected to have neutropenia (absolute neutrophil count < 500 cells/µl) for 10 or more days. Children (including neonates) and adolescents < 16 years of agetreatment of invasive candidiasis. prophylaxis of Candida infection in patients undergoing allogeneic haematopoietic stem-cell transplantation or patients who are expected to have neutropenia (absolute neutrophil count < 500 cells/µl) for 10 or more days. The decision to use Mycamine should take into account a potential risk for the development of liver tumours. Mycamine should therefore only be used if other antifungals are not appropriate. |
| Molecular Formula |
C56H70N9NAO23S
|
|---|---|
| Molecular Weight |
1292.26
|
| Exact Mass |
1291.42
|
| Elemental Analysis |
C, 52.05; H, 5.46; N, 9.76; Na, 1.78; O, 28.48; S, 2.48
|
| CAS # |
208538-73-2
|
| Related CAS # |
Micafungin;235114-32-6
|
| PubChem CID |
23666118
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
15
|
| Hydrogen Bond Acceptor Count |
24
|
| Rotatable Bond Count |
18
|
| Heavy Atom Count |
90
|
| Complexity |
2580
|
| Defined Atom Stereocenter Count |
15
|
| SMILES |
O=C1[C@@]([H])(NC([C@@]([H])(NC([C@]2([H])C[C@H](CN2C([C@@]([H])(NC([C@H](C[C@H]([C@H](NC([C@]2([H])[C@H]([C@H](CN21)C)O)=O)O)O)NC(C1C=CC(C2=NOC(C3C=CC(=CC=3)OCCCCC)=C2)=CC=1)=O)=O)[C@H](O)C)=O)O)=O)[C@H](O)[C@H](C1C=CC(=C(C=1)OS(O)(=O)=O)O)O)=O)[C@H](O)CC(=O)N.[Na]
|
| InChi Key |
KOOAFHGJVIVFMZ-WZPXRXMFSA-M
|
| InChi Code |
InChI=1S/C56H71N9O23S.Na/c1-4-5-6-17-86-32-14-11-28(12-15-32)39-21-33(63-87-39)27-7-9-29(10-8-27)49(75)58-34-20-38(70)52(78)62-54(80)45-46(72)25(2)23-65(45)56(82)43(37(69)22-41(57)71)60-53(79)44(48(74)47(73)30-13-16-36(68)40(18-30)88-89(83,84)85)61-51(77)35-19-31(67)24-64(35)55(81)42(26(3)66)59-50(34)76;/h7-16,18,21,25-26,31,34-35,37-38,42-48,52,66-70,72-74,78H,4-6,17,19-20,22-24H2,1-3H3,(H2,57,71)(H,58,75)(H,59,76)(H,60,79)(H,61,77)(H,62,80)(H,83,84,85);/q;+1/p-1/t25-,26+,31+,34-,35-,37+,38+,42-,43-,44-,45-,46-,47-,48-,52+;/m0./s1
|
| Chemical Name |
sodium 5-((1S,2S)-2-((2R,6S,9S,11R,12R,14aS,15S,16S,20S,23S,25aS)-20-((R)-3-amino-1-hydroxy-3-oxopropyl)-2,11,12,15-tetrahydroxy-6-((R)-1-hydroxyethyl)-16-methyl-5,8,14,19,22,25-hexaoxo-9-(4-(5-(4-(pentyloxy)phenyl)isoxazol-3-yl)benzamido)tetracosahydro-1H-dipyrrolo[2,1-c:2',1'-l][1,4,7,10,13,16]hexaazacyclohenicosin-23-yl)-1,2-dihydroxyethyl)-2-hydroxyphenyl sulfate
|
| Synonyms |
FK463; FK 463; FK-463; Funguard; Mycamine; FK463; Micafungin Na; FK463 Sodium; Micafungin sodium salt; Micafungin sodium
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : 32 ~100 mg/mL (24.76 ~77.38 mM )
Water : ~100 mg/mL (~77.38 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.93 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: ≥ 2.5 mg/mL (1.93 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (1.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (1.93 mM) Solubility in Formulation 5: 50 mg/mL (38.69 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Solubility in Formulation 6: 50 mg/mL (38.69 mM) in Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7738 mL | 3.8692 mL | 7.7384 mL | |
| 5 mM | 0.1548 mL | 0.7738 mL | 1.5477 mL | |
| 10 mM | 0.0774 mL | 0.3869 mL | 0.7738 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04728971 | NOT YET RECRUITING | Drug:Micafungin Sodium 50 MG Injection Drug:Caspofungin Acetate |
Liver Transplantation | Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine |
2022-10-01 | Phase 4 |
| NCT05784844 | RECRUITING | Drug:Meropenem Drug:Micafungin |
Febrile Neutropenia | Wake Forest University Health Sciences |
2024-08 | Phase 4 |
| NCT04738955 | UNKNOWN STATUS | Drug:Micafungin Sodium | Hematological Tumors Patients With High Risk Factors of Invasive Fungal Disease |
Shandong Provincial Hospital | 2021-02-01 | Phase 4 |
| NCT02678598 | COMPLETED | Drug:Micafungin | Invasive Fungal Infections | Astellas Pharma China,Inc. | 2015-03 | |
| NCT03174457 | COMPLETED | Drug:Micafungin | Invasive Fungal Infections | Astellas Pharma Singapore Pte.Ltd. | 2017-06-21 |
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
