| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
Pristinamycin targets the bacterial ribosome, inhibiting protein synthesis. Pristinamycin I (a macrolide) binds to the 50S ribosomal subunit, while Pristinamycin II (a streptogramin A) binds to a different site on the 50S subunit. The combination of the two components results in synergistic antibacterial activity, with the streptogramin A component causing a conformational change that enhances the binding of the streptogramin B component. This dual targeting mechanism makes pristinamycin effective against bacteria that are resistant to other antibiotics. Its primary target is the bacterial ribosome, which is essential for protein synthesis and bacterial survival.
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| ln Vitro |
Pristinamycin inhibits Staphylococci and Streptococci, including organisms that are extremely resistant to erythromycin, when applied at a concentration of less than or equal to 0.78 mg/l, according to in-vitro studies[2].
In vitro studies demonstrate that Pristinamycin is highly active against a broad spectrum of Gram-positive bacteria, including antibiotic-resistant strains such as MRSA and VRSA. The compound's antibacterial activity is assessed using standard broth microdilution or agar dilution methods to determine minimum inhibitory concentrations (MIC). The synergistic activity of the two components is confirmed by checkerboard assays, demonstrating fractional inhibitory concentration indices indicative of synergy. Pristinamycin's in vitro activity is bactericidal against susceptible strains. Its activity against Gram-negative bacteria is limited due to the outer membrane permeability barrier. |
| ln Vivo |
In order to investigate pristinamycin activity in vivo, C. psittaci was infected IP in mice. Seventy percent of the control group died. Pristinamycin was given to three groups of mice at doses of 25 mg/kg, 50 mg/kg, and 100 mg/kg, respectively. The therapeutic dosage of 100 mg/kg of the antibiotic was shown to be effective[3].
In vivo, Pristinamycin is an orally active antibiotic that has been used clinically for the treatment of Gram-positive infections, including those caused by MRSA. The compound's in vivo efficacy has been demonstrated in animal models of infection and in clinical studies. Following oral administration, the compound is absorbed and distributed to tissues, achieving therapeutic concentrations at sites of infection. Its in vivo activity is assessed in murine models of systemic infection, where treated animals show improved survival and reduced bacterial burden in target organs. The compound's clinical use has been established for the treatment of skin and soft tissue infections, respiratory tract infections, and other Gram-positive infections. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Pristinamycin involve measuring its binding to the bacterial ribosome and inhibition of protein synthesis. The assay typically uses purified bacterial ribosomes or cell-free translation systems. The compound is incubated with ribosomes and a labeled aminoacyl-tRNA or a reporter mRNA encoding a luciferase or fluorescent protein. Protein synthesis is quantified by measuring incorporation of labeled amino acids or reporter activity. Binding affinity is assessed using radiolabeled pristinamycin in competitive binding assays with ribosomes. IC₅0 values for protein synthesis inhibition are calculated from dose-response curves.
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| Cell Assay |
Cellular assays for Pristinamycin are conducted using bacterial cultures to determine its antibacterial activity. Standard broth microdilution or agar dilution methods are used to determine minimum inhibitory concentrations (MIC) against various bacterial strains. Bacteria are cultured in appropriate media at 37degC for 18-24 hours in the presence of serial dilutions of the compound. The MIC is defined as the lowest concentration that inhibits visible bacterial growth. Time-kill assays are performed to determine the bactericidal kinetics, and synergy with other antibiotics is assessed using checkerboard assays. The compound's activity against biofilm-forming bacteria may also be evaluated using biofilm formation assays.
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| Animal Protocol |
In vivo animal studies with Pristinamycin are conducted in murine models of bacterial infection. Mice are infected with a lethal dose of a susceptible pathogen (e.g., S. aureus) via intraperitoneal or intravenous injection. Treated animals receive the compound orally at various doses, and survival is monitored over several days. Bacterial burden in target organs (e.g., spleen, liver, kidneys) is determined by plating serial dilutions of tissue homogenates. The compound's efficacy is compared to that of standard antibiotics. Pharmacokinetic studies are also performed to determine oral bioavailability, tissue distribution, and elimination.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Pristinamycin have been characterized in preclinical and clinical studies. The compound is orally bioavailable, making it suitable for oral administration. Following oral absorption, the two components (PI and PII) are distributed to various tissues. The compound has a molecular weight of approximately 1349.48 g/mol and a molecular formula of C₇1H₈4N10O1₇. It is metabolized in the liver and excreted via bile and urine. The compound's half-life and other PK parameters have been determined in pharmacokinetic studies. The compound is typically stored at -20degC.
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| Toxicity/Toxicokinetics |
Toxicological data for Pristinamycin have been characterized in preclinical studies and clinical use. The compound is generally well-tolerated at therapeutic doses, with gastrointestinal disturbances being the most common adverse effects. Allergic reactions may occur in susceptible individuals. The compound is not recommended for use in patients with known hypersensitivity to streptogramins. In preclinical toxicology studies, the compound showed no significant genotoxicity or carcinogenicity. The compound's safety profile is well-established from its clinical use as an oral antibiotic.
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| References |
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| Additional Infomation |
Pristinamycin is an oral streptogramin antibiotic used for the treatment of Gram-positive infections, including those caused by MRSA. It is a complex of two components, Pristinamycin I and Pristinamycin II, which act synergistically to inhibit bacterial protein synthesis. The compound is highly active against many antibiotic-resistant pathogens. It is not available in all countries but is used in some regions for the treatment of skin and soft tissue infections, respiratory tract infections, and other Gram-positive infections. The compound is an FDA-approved drug in some jurisdictions and has clinical indications for the treatment of Gram-positive bacterial infections.
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| Molecular Formula |
C73H89N11O17
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| Molecular Weight |
1392.55
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| Exact Mass |
866.396
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| CAS # |
270076-60-3
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| Related CAS # |
Pristinamycin IA;3131-03-1;Virginiamycin M1;21411-53-0
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| PubChem CID |
155887675
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
1202.1±65.0 °C at 760 mmHg
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| Flash Point |
680.8±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.650
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| LogP |
-0.45
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
39
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
199
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| Complexity |
4340
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| Defined Atom Stereocenter Count |
10
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 0.7181 mL | 3.5905 mL | 7.1811 mL | |
| 5 mM | 0.1436 mL | 0.7181 mL | 1.4362 mL | |
| 10 mM | 0.0718 mL | 0.3591 mL | 0.7181 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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