Amphomycin |
Catalog No.GC15221
One-Click Copy Product Info
|
natural antibacterial lipopeptide
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1402-82-0
Sample solution is provided at 25 µL, 10mM.
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Amphomycin is a natural antibacterial lipopeptide.
Cyclic lipopeptides are a promising class of natural products with antibiotic properties. Cyclic lipopeptides are amphiphilic molecules, composed of a fatty acid tail linked to a short oligopeptide which form a macrocylic ring structure.
In vitro: In previous study, Calf brain endoplasmic reticulum membranes were incubated with varying concentrations of GDP-mannose in the presence and absence of amphomycin, results showed no significant difference in apparent Km for GDP-mannose. However, the Vmax was reduced in the presence of amphomycin as compared with in its absence. Moreover, when mannosylphosphoryldolichol synthase activity was measured in the presence of amphomycin, the shape of the substrate velocity curve changed from a rectangular hyperbola to a sigmoid [1].
In vivo: The PK of lipopeptides, the semi-synthetic amphomycin analogues, were evaluated in mice and rats following single i.v. and oral administration. Following oral administration at 50 mg/kg, plasma concentrations of amphomycin analogues were <0.3-0.9 μg/mL, indicating that oral availability was low. Following i.v. administration (5-10 mg/kg), the majority of lipopeptides demonstrated a long half-life, low clearance and a volume of distribution indicative of extracellular penetration. The long half-life and low clearance indicated that drug serum concentrations remained above the target minimal inhibitory concentration levels for significant periods of time. When combined with the potent efficacy against Gram-positive organisms, the results supported further development of these lipopeptide analogues towards clinical evaluation [2].
Clinical trial: Up to now, amphomycin is still in the preclinical development stage.
References:
[1] D. K. Banerjee. Amphomycin inhibits mannosylphosphoryldolichol synthesis by forming a complex with dolichylmonophosphate. The Journal of Biological Chemisty 264(4), 2024-2028 (1989).
[2] Pasetka CJ, Erfle DJ, Cameron DR, Clement JJ, Rubinchik E. Novel antimicrobial lipopeptides with long in vivo half-lives. Int J Antimicrob Agents. 2010 Feb;35(2):182-5.
| Cas No. | 1402-82-0 | SDF | |
| Chemical Name | 2,2'-((6S,9R,15S,21S,24S,26aR,33S,34R,36aS)-9-((R)-1-aminoethyl)-33-((2S)-3-carboxy-2-((Z)-10-methyldodec-3-enamido)propanamido)-24-((S)-1-carboxyethyl)-6-isopropyl-34-methyl-5,8,11,14,17,20,23,26,32,36-decaoxotetratriacontahydro-1H,5H-pyrido[1,2-a]pyrrol | ||
| Canonical SMILES | O=C([C@@H]1N(CCCC1)C([C@@](NC([C@@H](NC(C/C=C\CCCCCC(CC)C)=O)CC(O)=O)=O)([C@H](NC([C@@H]2CCCN2C([C@@H](NC([C@@]([H])([C@H](N)C)N3)=O)C(C)C)=O)=O)C)[H])=O)N[C@@]([C@@H](C(O)=O)C)(C(N[C@H](C(NCC(N[C@@H](CC(O)=O)C(NCC3=O)=O)=O)=O)CC(O)=O)=O)[H] | ||
| Formula | C58H91N13O20 | M.Wt | 1290.4 |
| Solubility | DMF: Soluble,DMSO: Soluble,Ethanol: Soluble,Methanol: Soluble | Storage | Store at -20°C |
| 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 | 775 μL | 3.8748 mL | 7.7495 mL |
| 5 mM | 155 μL | 775 μL | 1.5499 mL |
| 10 mM | 77.5 μL | 387.5 μL | 775 μL |
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 saline, 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: >95.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)