Amphotericin B (Synonyms: LNSAmB, NSC 527017) |
| Catalog No.GC14092 |
Antibiotique polyène amphipathique
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1397-89-3
Sample solution is provided at 25 µL, 10mM.
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Amphotericin B, a polyene antifungal antibiotic, has been produced from a strain of Streptomyces nodosus with an IC50 of 0.028–0.290 μg/ml.
In vitro: Amphotericin B was the most effective drug for treating many life-threatening fungal infections. In cells expressing TLR2 and CD14, amphotericin B induced signal transduction and inflammatory cytokine release. In primary murine macrophages and human cell lines expressing TLR2, CD14, and the adapter protein MyD88, amphotericin induced NF-κB-dependent reporter activity and cytokine release, whereas cells deficient in any of these failed to respond. Cells with TLR4 mutation were less responsive to amphotericin B stimulation than cells expressing normal TLR4 [1]. Amphotericin B could interact with cholesterol, the major sterol of mammal membranes, thus limiting the usefulness of Amphotericin B due to its relatively high toxicity [2]. Low AmB concentrations (≤ 0.1 μM) induced a polarization potential in KCl-loaded liposomes suspended in an iso-osmotic sucrose solution, indicating K+ leakage. AmB (＞ 0.1 μM) allowed cations and anions movements. LPs suspended in an iso-osmotic NaCl solution and exposed to AmB (0.05 μM) exhibited a nearly total collapse of the negative membrane potential, indicated that Na+ entered into the cells [3].
In vivo: Amphotericin B prolonged the incubation time and decreased PrPSc accumulation in the hamster scrapie model. Amphotericin B markedly resulted in reduction of PrPSc levels in mice with transmissible subacute spongiform encephalopathies (TSSE) [4].
References:
[1]. Sau K1,Mambula SS,Latz E,Henneke P,Golenbock DT,Levitz SM.The antifungal drug amphotericin B promotes inflammatory cytokine release by a Toll-like receptor- and CD14-dependent mechanism.J Biol Chem.2003 Sep 26;278(39):37561-8. Epub 2003 Jul 14.
[2]. Barwicz J1,Tancrède P.The effect of aggregation state of amphotericin-B on its interactions with cholesterol- or ergosterol-containing phosphatidylcholine monolayers.Chem Phys Lipids.1997 Feb 28;85(2):145-55.
[3]. Ramos H1,Valdivieso E,Gamargo M,Dagger F,Cohen BE.Amphotericin B kills unicellular leishmanias by forming aqueous pores permeable to small cations and anions.J Membr Biol.1996 Jul;152(1):65-75.
[4]. Demaimay R1,Adjou K,Lasmézas C,Lazarini F,Cherifi K,Seman M,Deslys JP,Dormont D.Pharmacological studies of a new derivative of amphotericin B, MS-8209, in mouse and hamster scrapie.J Gen Virol.1994 Sep;75 ( Pt 9):2499-503.
| Cell experiment [1]: | |
|
Cell lines |
peritoneal macrophages; HEK293 cells expressing TLR2 and CD14 |
|
Preparation method |
The solubility of this compound in DMSO is >46.2mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
1, 2, and 4 μg/ml |
|
Applications |
In peritoneal macrophages from CD14 knockout mice (C57BL/6 CD14–/–) and CD14 wild-type (C57BL/6 CD14+/+) mice, Amphotericin B failed to induce the production of TNF-α in macrophages from CD14–/– mice. HEK293 cells expressing TLR2 and CD14 responded more strongly to Amphotericin B (1, 2, and 4 μg/ml). |
| Animal experiment [2]: | |
|
Animal models |
hamster scrapie model |
|
Dosage form |
2.5 mg/kg; p.i. injection from 0 to 7 days |
|
Application |
In hamsters infected intracerebrally with scrapie, Amphotericin B significantly prolonged the survival time by 14.7 days. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Sau K1,Mambula SS,Latz E,Henneke P,Golenbock DT,Levitz SM.The antifungal drug amphotericin B promotes inflammatory cytokine release by a Toll-like receptor- and CD14-dependent mechanism.J Biol Chem.2003 Sep 26;278(39):37561-8. Epub 2003 Jul 14. [2]. Demaimay R1,Adjou K,Lasmézas C,Lazarini F,Cherifi K,Seman M,Deslys JP,Dormont D.Pharmacological studies of a new derivative of amphotericin B, MS-8209, in mouse and hamster scrapie.J Gen Virol.1994 Sep;75 ( Pt 9):2499-503. |
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| Cas No. | 1397-89-3 | SDF | |
| Synonymes | LNSAmB, NSC 527017 | ||
| Canonical SMILES | CC1C=CC=CC=CC=CC=CC=CC=CC(CC2C(C(CC(O2)(CC(CC(C(CCC(CC(CC(=O)OC(C(C1O)C)C)O)O)O)O)O)O)O)C(=O)O)OC3C(C(C(C(O3)C)O)N)O | ||
| Formula | C47H73NO17 | M.Wt | 924.08 |
| Solubility | ≥ 46.2mg/mL in DMSO | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.0822 mL | 5.4108 mL | 10.8216 mL |
| 5 mM | 0.2164 mL | 1.0822 mL | 2.1643 mL |
| 10 mM | 0.1082 mL | 0.5411 mL | 1.0822 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
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