| Size | Price | Stock | Qty |
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| 5mg |
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| 25mg |
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| Targets |
Nosiheptide inhibits bacterial protein synthesis by interfering with the function of elongation factors. It binds to the 50S ribosomal subunit and prevents the translocation step of protein synthesis. This mechanism is characteristic of thiopeptide antibiotics and results in bacteriostatic or bactericidal activity against a range of Gram-positive bacteria.
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| ln Vitro |
Nosiheptide demonstrated substantial efficacy against all modern S. MIC values ≤ 0.25 mg/L were found for several drug-resistant clinical isolates among the tested aureus strains. Nosiheptide was inert against the majority of tested Gram-negative germs, however it was quite active against Enterococcus species and modern, highly virulent Clostridium difficile BI strains. Nosiheptide was able to rapidly kill Staphylococcus aureus in a concentration- and time-dependent manner, achieving over 2 log killing rates at 10X MIC in under 6 hours, according to time-kill study. Moreover, it was discovered that nosiheptide's anti-S and noncytotoxic at >> 100X MIC to mammalian cells. Twenty percent human serum did not inhibit aureus activity. Notably, nosiheptide showed considerably longer post-antibiotic effects than vancomycin did against Staphylococcus aureus linked to healthcare and the community [1].
Nosiheptide is effective against many different methicillin-resistant Staphylococcus aureus (MRSA) strains with minimum inhibitory concentrations (MICs) ≤ 0.25 mg/L. It has broad-spectrum activity against other Gram-positive bacteria. The compound's antibacterial activity is routinely assessed using broth microdilution or agar dilution methods to determine MIC values against various bacterial strains. |
| ln Vivo |
In female CD1 mice, nosiheptide (20 mg/kg; i.p.; 1 and 8 h postinfection) dramatically reduced mortality. Six out of ten mice in the control group perished on day one, whereas ten mice receiving nosiheptide were still alive on day three [1].
Nosiheptide is used in vivo as a feed additive for animal growth. It promotes weight gain and improves feed efficiency in chickens and other livestock. The antibiotic's use as a growth promoter is based on its ability to modulate the gut microbiota and reduce the incidence of subclinical infections in production animals. |
| Enzyme Assay |
Nosiheptide's antibacterial activity can be evaluated using standard microbiological assays in cell-free systems. The compound's effect on protein synthesis can be assessed using in vitro translation assays with bacterial lysates (e.g., E. coli S30 extract) and a reporter mRNA (e.g., luciferase). The inhibition of protein synthesis by nosiheptide is measured by quantifying the reduction in reporter activity.
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| Cell Assay |
In vitro cellular assays for nosiheptide involve treating bacterial cultures (e.g., S. aureus, including MRSA strains) with the compound and assessing growth inhibition. The minimum inhibitory concentration (MIC) is determined by broth microdilution according to CLSI guidelines. Time-kill assays are used to assess the bactericidal or bacteriostatic nature of the compound's activity.
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| Animal Protocol |
Animal/Disease Models: Eightweeks old female CD1 mice were injected with HA-Staphylococcus aureus strain Sanger 252[1].
Doses: 20 mg/kg. Route of Administration: intraperitoneal (ip) injection; intraperitoneal (ip) injection. Injection results at 1 hour and 8 hrs (hrs (hours)) after infection: Provided significant protection against death. In vivo animal experiments with nosiheptide are conducted primarily in livestock animals (chickens, pigs) to evaluate its efficacy as a growth promoter. Animals are fed diets containing nosiheptide at various concentrations, and weight gain, feed conversion ratio, and health status are monitored. The compound's effects on the gut microbiota and its potential for selecting for antibiotic resistance are also studied. |
| ADME/Pharmacokinetics |
Nosiheptide has a molecular weight of 1222.36 and a molecular formula of C₅₁H₄₃N₁₃O₁₂S₆. It is a solid at room temperature and is typically stored at -20°C. Purity is typically ≥95%. The compound is soluble in DMSO and other organic solvents. It is stable under recommended storage conditions and is protected from light and moisture.
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| Toxicity/Toxicokinetics |
Nosiheptide is generally considered to have low toxicity in animals at the concentrations used as a feed additive. However, its use as a growth promoter has raised concerns about the potential for selection of antibiotic-resistant bacteria. The compound is not approved for use in human medicine.
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| References |
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| Additional Infomation |
Nosiheptide has been reported to be detected in both Streptomyces actuosus and Streptomyces griseosporeus, and relevant data are available for reference. See also: Nusiti (note moved to).
Nosiheptide is a thiopeptide antibiotic used as a feed additive for animal growth. It is effective against Gram-positive bacteria, including MRSA. The compound inhibits bacterial protein synthesis. It is available from various commercial suppliers for research and analytical applications. |
| Molecular Formula |
C51H51N13O12S6
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|---|---|
| Molecular Weight |
1230.4
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| Exact Mass |
1221.147
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| Elemental Analysis |
C, 49.79; H, 4.18; N, 14.80; O, 15.60; S, 15.63
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| CAS # |
56377-79-8
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| Related CAS # |
56377-79-8;
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| PubChem CID |
16129696
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Melting Point |
310-320° (dec)
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| Index of Refraction |
1.699
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| LogP |
0.72
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
24
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
82
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| Complexity |
2510
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| Defined Atom Stereocenter Count |
0
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| SMILES |
NC(C(NC(C1=CSC(C2C(O)=CC3C4SC=C(C(NC(C(N/C(/C5SC=C(C(NC6CC(O)C(=O)OCC7=C8C(NC(=C8C)C(=O)SCC(C8SC=C(C=3N=2)N=8)NC(=O)C2=CSC6=N2)=CC=C7)=O)N=5)=C\C)=O)C(O)C)=O)N=4)=N1)=O)=C)=O
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| InChi Key |
OQAOHXRUMXWDLQ-ATVZKCIHSA-N
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| InChi Code |
1S/C51H43N13O12S6/c1-5-23-46-60-28(14-79-46)41(70)56-25-10-33(67)50(74)76-11-21-7-6-8-24-34(21)18(2)35(54-24)51(75)82-17-31(57-42(71)29-15-80-47(25)61-29)48-58-26(12-78-48)37-22(45-59-30(13-77-45)43(72)64-36(20(4)65)44(73)55-23)9-32(66)38(63-37)49-62-27(16-81-49)40(69)53-19(3)39(52)68/h5-9,12-16,20,25,31,33,36,54,65-67H,3,10-11,17H2,1-2,4H3,(H2,52,68)(H,53,69)(H,55,73)(H,56,70)(H,57,71)(H,64,72)/b23-5-/t20-,25+,31+,33+,36+/m1/s1
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| Chemical Name |
A name could not be generated for this structure.
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| Synonyms |
Nosiheptide; Multhiomycin; Multiomycin; Nosiheptidum; RP 9671; RP-9671; RP9671;
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~81.81 mM)
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| 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 | 0.8127 mL | 4.0637 mL | 8.1274 mL | |
| 5 mM | 0.1625 mL | 0.8127 mL | 1.6255 mL | |
| 10 mM | 0.0813 mL | 0.4064 mL | 0.8127 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.
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