Nosiheptide (Synonyms: Multhiomycin,NSC 307240,RP 9671) |
| Catalog No.GC16572 |
Nosiheptide (multiomicina), un antibiÓtico tiopéptido producido por Streptomyces actuosus, inhibe la sÍntesis de proteÍnas bacterianas y tiene un sistema de anillo lateral de indol Único y grupos hidroxilo regioespecÍficos en el nÚcleo macrocÍclico caracterÍstico.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 56377-79-8
Sample solution is provided at 25 µL, 10mM.
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MIC: ≤ 0.25 mg/L for methicillin-resistant S. aureus strains; ≤ 0.125 mg/L for Enterococcus spp; 0.008 mg/L for BI strain of C. difficile
Nosiheptide is a thiopeptide antibiotic.
Thiopeptides are a family of antibiotics counting with more than one hundred different entities. Although thiopeptides are mainly isolated from soil bacteria, new members have been isolated from marine samples. Thiopeptides have been reported to have a wide range of biological properties, such as antiplasmodial, anticancer, immunosuppressive, etc.
In vitro: The mode of action of nosiheptide on bacterial protein synthesis was found to be closely similar to that of thiostrepton. Both antibiotics could inhibit functions of elongation factors Tu and G and could also significantly reduce the synthesis of guanosine penta- and tetraphosphates to stringent factor. In addition, the actinomycetes that produced nosiheptide were able to defend themselves against their products in similar fashion, which involved specific pentosemethylation of 23s ribosomal RNA [1].
In vivo: The rHDL–nosiheptide complex was intravenously administered to male Wistar rats and the distribution of nosiheptide in the liver and plasma was monitored 30 min after injection. Results showed that the hepatic distribution of the rHDL–nosiheptide complex accounted for most of the administered nosiheptide, and was seven times as much as that in plasma. These findings indicated that the rHDL–nosiheptide complex could targete nosiheptide to the liver [2].
Clinical trial: Up to now, nosiheptide is still in the preclinical development stage.
References:
[1] E. Cundliffe and J. Thompson. The mode of action of nosiheptide (multhiomycin) and the mechanism of resistance in the producing organism. J.Gen.Microbiol. 126(1), 185-192 (1981).
[2] Feng M, Cai Q, Shi X, Huang H, Zhou P, Guo X. Recombinant high-density lipoprotein complex as a targeting system of nosiheptide to liver cells. J Drug Target. 2008 Jul;16(6):502-8.
| Cas No. | 56377-79-8 | SDF | |
| Sinónimos | Multhiomycin,NSC 307240,RP 9671 | ||
| Chemical Name | N-[1-(aminocarbonyl)ethenyl]-2-[(11S,14Z,21S,23S,29S)-14-ethylidene-9,10,11,12,13,14,19,20,21,22,23,24,26,33,35,36-hexadecahydro-3,23-dihydroxy-11-[(1R)-1-hydroxyethyl]-31-methyl-9,12,19,24,33,43-hexaoxo-30,32-imino-8,5:18,15:40,37-trinitrilo-21,36-([2,4] | ||
| Canonical SMILES | OC1=C(C2=NC(C(NC(C(N)=O)=C)=O)=CS2)N=C(C3=CSC([C@](NC(C4=CSC([C@](NC(C5=CSC(/C(NC([C@](NC(C6=CSC7=N6)=O)([H])[C@@H](O)C)=O)=C/C)=N5)=O)([H])C[C@H](O)C(OC8)=O)=N4)=O)([H])CSC(C9=C(C)C(C8=CC=C%10)=C%10N9)=O)=N3)C7=C1 | ||
| Formula | C51H43N13O12S6 | M.Wt | 1222.4 |
| 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. |
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| 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 | 0.8181 mL | 4.0903 mL | 8.1806 mL |
| 5 mM | 0.1636 mL | 0.8181 mL | 1.6361 mL |
| 10 mM | 0.0818 mL | 0.409 mL | 0.8181 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)
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