| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| Other Sizes |
Purity: ≥70%
| Targets |
Echinocandin B targets the synthesis of β(1,3)-D-glucan, an essential component of the fungal cell wall. It acts by inhibiting the enzyme β-(1,3)-D-glucan synthase, which is crucial for the synthesis of β-glucan in fungal cell walls. By obstructing this enzyme, Echinocandin B disrupts fungal cell wall integrity, leading to cell lysis and death.
|
|---|---|
| ln Vitro |
Echinocandin B belongs to lipopeptide antifungal antibiotic bearing five types of direct precursor amino acids including proline, ornithine, tyrosine, threonine, and leucine. The objective of this study is to screen over-producing mutant in order to improve echinocandin B production; a stable mutant Aspergillus nidulans ZJB12073, which can use fructose as optimal carbon source instead of expensive mannitol, was selected from thousand isolates after several cycles of UV and microwave irradiation in turn. The results showed that mutant strain ZJB12073 exhibited 1.9-fold improvement in echinocandin B production to 1656.3 ± 40.3 mg/L when compared with the parent strain. Furthermore, the effects of precursor amino acids and some chemicals on echinocandin B biosynthesis in A. nidulans were investigated, respectively. Tyrosine, leucine, and biotin were selected as key factors to optimize the medium employing uniform design method. The results showed that the optimized fermentation medium provided another 63.1 % increase to 2701.6 ± 31.7 mg/L in final echinocandin B concentration compared to that of unoptimized medium.[2]
In vitro, Echinocandin B exhibits potent antifungal activity against a wide range of pathogenic fungi. It has been found to be highly effective against Candida and Aspergillus species. As a naturally occurring lipopeptide, it demonstrates significant antifungal properties. The compound's activity has been characterized in broth microdilution assays to determine minimum inhibitory concentrations (MICs) against various fungal strains. |
| ln Vivo |
Echinocandin B has been found to be effective against a wide range of fungal infections in vivo. It has also been found to have a low toxicity profile, making it a safe and effective antifungal agent. As a naturally occurring compound, it serves as a lead for the development of semi-synthetic echinocandin antifungals such as caspofungin, micafungin, and anidulafungin.
|
| Enzyme Assay |
The β-glucan synthase inhibition assay for Echinocandin B involves incubating the compound with fungal membrane preparations containing β-(1,3)-D-glucan synthase and the substrate UDP-glucose. The reaction is carried out in an assay buffer at 30°C for a specified time. The incorporation of [¹⁴C]-glucose into β-glucan is measured by scintillation counting. IC50 values for inhibition of glucan synthase activity are calculated from dose-response curves.
|
| Cell Assay |
To evaluate the antifungal activity of Echinocandin B, fungal strains (such as Candida albicans or Aspergillus fumigatus) are cultured in appropriate growth medium. Broth microdilution assays are performed in 96-well plates with two-fold serial dilutions of Echinocandin B. Fungal suspensions are added to achieve a final inoculum of approximately 1-5 × 10³ CFU/mL. Plates are incubated at 35-37°C for 24-48 hours, and the MIC is determined as the lowest concentration that inhibits visible fungal growth.
|
| Animal Protocol |
The in vivo efficacy of Echinocandin B is evaluated in animal models of fungal infection, such as mouse models of systemic candidiasis or aspergillosis. Immunocompetent or immunosuppressed mice are infected with a fungal pathogen via intravenous or intraperitoneal injection. After infection, mice are treated with Echinocandin B at various doses, typically administered intravenously or intraperitoneally. Survival rates and fungal burden in target organs are measured.
|
| ADME/Pharmacokinetics |
Specific pharmacokinetic data for Echinocandin B are not detailed in the available sources. The compound has a molecular weight of 1060.40 and is a naturally occurring lipopeptide. As a lead compound for semi-synthetic echinocandins, its pharmacokinetic properties have been characterized in preclinical studies. Echinocandin B is typically stored as a powder at -20°C for long-term stability.
|
| Toxicity/Toxicokinetics |
Echinocandin B has been found to have a low toxicity profile, making it a safe and effective antifungal agent. As a research compound, it is intended for laboratory use only and is not approved for human therapeutic applications. The compound is a potent antifungal that acts by inhibition of the synthesis of β(1,3)-D-glucan. Standard safety precautions should be followed when handling this compound.
|
| References | |
| Additional Infomation |
Echinocandin B is a cyclic hexapeptide echinocandin antibiotic isolated from Aspergillus nidulans var. echinulatus. It possesses specific anti-yeast activity and can be used as an anti-infective agent. Echinocandin B has also been reported to exist in Streptomyces, Aspergillus spinulosporus, and Aspergillus nidulans, and relevant data are available for reference.
Echinocandin B is a potent, naturally occurring lipopeptide antifungal compound produced by Aspergillus nidulans. It inhibits β-(1,3)-D-glucan synthase, an enzyme crucial for fungal cell wall synthesis. It is highly effective against Candida and Aspergillus species and has a low toxicity profile. It serves as a lead compound for the development of semi-synthetic echinocandin antifungals. |
| Molecular Formula |
C52H81N7O16
|
|---|---|
| Molecular Weight |
1060.2
|
| Exact Mass |
1059.57
|
| CAS # |
54651-05-7
|
| PubChem CID |
9898144
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
0.251
|
| Hydrogen Bond Donor Count |
14
|
| Hydrogen Bond Acceptor Count |
16
|
| Rotatable Bond Count |
20
|
| Heavy Atom Count |
75
|
| Complexity |
1940
|
| Defined Atom Stereocenter Count |
15
|
| SMILES |
OC1C2C(NC(C(CC(C(NC(C(C)O)C(N3CC(CC3C(NC(C(C(C3C=CC(=CC=3)O)O)O)C(NC(C(C)O)C(N2CC1C)=O)=O)=O)O)=O)=O)NC(CCCCCCCC=CCC=CCCCCC)=O)O)O)=O
|
| InChi Key |
FAUOJMHVEYMQQG-HVYQDZECSA-N
|
| InChi Code |
1S/C52H81N7O16/c1-5-6-7-8-9-10-11-12-13-14-15-16-17-18-19-20-38(65)53-35-26-37(64)48(71)57-50(73)42-43(66)29(2)27-59(42)52(75)40(31(4)61)55-49(72)41(45(68)44(67)32-21-23-33(62)24-22-32)56-47(70)36-25-34(63)28-58(36)51(74)39(30(3)60)54-46(35)69/h9-10,12-13,21-24,29-31,34-37,39-45,48,60-64,66-68,71H,5-8,11,14-20,25-28H2,1-4H3,(H,53,65)(H,54,69)(H,55,72)(H,56,70)(H,57,73)/b10-9-,13-12-/t29-,30+,31+,34+,35-,36-,37+,39-,40-,41-,42-,43-,44-,45-,48+/m0/s1
|
| Chemical Name |
(9Z,12Z)-N-((2R,6S,9S,11R,12R,14aS,15S,16S,20S,23S,25aS)-23-((1S,2S)-1,2-dihydroxy-2-(4-hydroxyphenyl)ethyl)-2,11,12,15-tetrahydroxy-6,20-bis((R)-1-hydroxyethyl)-16-methyl-5,8,14,19,22,25-hexaoxotetracosahydro-1H-dipyrrolo[2,1-c:2',1'-l][1,4,7,10,13,16]hexaazacyclohenicosin-9-yl)octadeca-9,12-dienamide
|
| Synonyms |
A30912A; A 30912A; A-30912A; A22082; A 22082; A-22082; Echinocandin B; NSC 287461;
|
| 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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 0.9432 mL | 4.7161 mL | 9.4322 mL | |
| 5 mM | 0.1886 mL | 0.9432 mL | 1.8864 mL | |
| 10 mM | 0.0943 mL | 0.4716 mL | 0.9432 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA