| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
Ramoplanin targets the bacterial cell wall by binding to the lipid intermediate peptidoglycan precursor (lipid I and lipid II), which are essential for cell wall synthesis. Unlike vancomycin, which binds to the D-Ala-D-Ala terminus, ramoplanin interacts with the sugars and phosphate groups of lipid II, inhibiting the transglycosylation step in peptidoglycan assembly. This blocks the formation of the cell wall, leading to osmotic lysis and bacterial death. It has potent activity against C. difficile and is used in clinical development for treating Clostridium difficile-associated diarrhea (CDAD).
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| ln Vitro |
By means of the fermentation of Fermentation Inhibitor II synthetic peptide, ramoplanin demonstrates its bactericidal effect against both Gram fast aerobic and anaerobic bacteria [1].
In vitro, ramoplanin exhibits potent antibacterial activity with MIC₉₀ values ranging from 0.06 to 2 µg/mL against a wide range of Gram-positive bacteria, including MRSA and VRE. Time-kill studies show rapid bactericidal activity. It is also effective against spores of C. difficile, preventing their germination. The compound shows synergy with other antibiotics and has a low propensity for resistance development due to its unique target. It is inactive against Gram-negative bacteria due to the outer membrane barrier. |
| ln Vivo |
Ramoplanin (100, 500 μg/mL; vascular wall; for 8 days) reduces the amount of vancomycin-resistant enterococci (VRE) to undetectable levels during treatment[1].
In vivo, ramoplanin has been evaluated in animal models of C. difficile infection and in clinical trials. Oral administration in hamsters resulted in significantly reduced mortality and disease symptoms. In humans, oral ramoplanin (e.g., 100-200 mg twice daily) was shown to be effective in treating CDAD, with response rates comparable to vancomycin. Its systemic absorption after oral administration is minimal, which is advantageous for targeting intestinal infections. It is also being studied as a topical agent for skin infections. |
| Enzyme Assay |
In vitro susceptibility testing for ramoplanin follows CLSI guidelines using broth microdilution. MICs are determined for various Gram-positive organisms. The compound's activity against C. difficile spores is assessed by spore germination and outgrowth inhibition assays. The mechanism of action is confirmed by monitoring the incorporation of radiolabeled precursors into peptidoglycan and by electron microscopy to observe cell wall damage.
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| Cell Assay |
In vitro cellular experiments for ramoplanin are focused on its effect on C. difficile and other Gram-positive bacteria in cell culture models. The compound is added to bacterial cultures, and viability is assessed by colony counting. Its effect on toxin production (e.g., C. difficile toxins A and B) is measured by ELISA. The compound's activity in a human gut microbiome model is evaluated to assess its impact on the normal flora.
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| Animal Protocol |
Animal/Disease Models: Female CF1 mice (25-30) g) [1]
Doses: 100 μg/ml, 500 μg/ml Route of Administration: oral; lasted for 8 days Experimental Results: VRE levels were undetectable in feces during treatment. In vivo animal studies for ramoplanin are conducted in the hamster model of C. difficile infection. Hamsters are treated with antibiotics to induce susceptibility, then infected with C. difficile. Ramoplanin is administered orally. Disease severity (weight loss, diarrhea, mortality) is monitored. Intestinal bacterial counts and toxin levels are measured. Pharmacokinetic properties are determined from plasma and fecal samples. Safety is assessed by clinical observation and histopathology. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
No absorption/Limited absorption. The pharmacokinetic properties of ramoplanin are characterized by very low oral bioavailability (<1%) due to its large molecular size and hydrophilicity. It is not absorbed systemically but remains in the gastrointestinal tract, making it ideal for treating intestinal infections. When administered intravenously, it has a moderate half-life of 1-2 hours, but IV use is limited by toxicity. Its fecal concentrations are high after oral dosing. It is metabolized by intestinal bacteria and excreted in feces. |
| Toxicity/Toxicokinetics |
The toxicity profile of ramoplanin is manageable. Oral administration is well-tolerated, with no significant systemic toxicity. The most common adverse events are gastrointestinal (nausea, abdominal pain). Intravenous administration is associated with dose-limiting toxicity, including infusion reactions and nephrotoxicity, limiting its systemic use. It is not approved for IV use. No significant cardiotoxicity or genotoxicity has been reported.
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| References |
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| Additional Infomation |
Ramoplanin is a novel glycolipid antibiotic currently under development for the treatment of Clostridium difficile-associated diarrhea (CDAD). Ramoplanin has been discovered in the genus Actinoplanes, and relevant data have been reported. Indications: For the treatment of bacterial infections. Mechanism of Action: Ramoplanin is the first novel antibacterial drug to enter clinical trials. It is a glycolipid antibiotic produced by the fermentation of Actinoplanes spp. Ramoplanin blocks bacterial cell wall biosynthesis by interfering with peptidoglycan synthesis. Ramoplanin inhibits the conversion of lipid intermediate I to lipid intermediate II catalyzed by N-acetylglucosamine transferase, a step that occurs before transglycosylation and transpeptidation. Ramoplanin's mechanism of action differs from that of glycopeptide antibiotics. Unlike glycopeptides, Ramoplanin does not form a complex with the D-Ala–D-Ala sequence of cell wall precursors.
Ramoplanin is a promising antibiotic for the treatment of C. difficile-associated diarrhea and other Gram-positive infections. Its unique mechanism of action, targeting lipid II, provides activity against vancomycin-resistant strains. It has been granted orphan drug status and has completed Phase 2 clinical trials for CDAD. Its development has been pursued for oral and topical applications due to its favorable local safety profile. It represents a valuable addition to the antibiotic arsenal, particularly for resistant organisms. |
| Molecular Formula |
C106H170N21O30CL
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|---|---|
| Molecular Weight |
2254.0597
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| Exact Mass |
2552.035
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| CAS # |
76168-82-6
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| PubChem CID |
16132338
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Melting Point |
>218 °C(dec.)
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| Index of Refraction |
1.689
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| LogP |
-6.39
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| Hydrogen Bond Donor Count |
31
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| Hydrogen Bond Acceptor Count |
32
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| Rotatable Bond Count |
61
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| Heavy Atom Count |
158
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| Complexity |
4810
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| Defined Atom Stereocenter Count |
15
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O : ~33.33 mg/mL
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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 | 0.4436 mL | 2.2182 mL | 4.4364 mL | |
| 5 mM | 0.0887 mL | 0.4436 mL | 0.8873 mL | |
| 10 mM | 0.0444 mL | 0.2218 mL | 0.4436 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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