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500mg | ||
1g | ||
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ln Vitro |
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Studies involving the human use of drugs labeled with deuterium suggest that these compounds may offer some advantages when compared with their nondeuterated counterparts. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs. Deutetrabenazine is the first deuterated drug to receive Food and Drug Administration approval. This deuterated form of the drug tetrabenazine is indicated for the treatment of chorea associated with Huntington's disease as well as tardive dyskinesia. Ongoing clinical trials suggest that a number of other deuterated compounds are being evaluated for the treatment of human diseases and not merely as research tools. [1] Vancomycin is a large glycopeptide with a molecular weight of 1450 Da. [2] Vancomycin is a unique glycopeptide that is structurally unrelated to any currently available antibiotic. It also has a unique mode of action, inhibiting phase II cell wall synthesis in susceptible bacteria. Vancomycin is effective against a variety of Gram-positive bacteria, such as Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus agalactiae, Streptococcus bovis, Streptococcus mutans, Streptococcus viridans, and Enterococci [3].
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ln Vivo |
Vancomycin is a macromolecular glycopeptide with a molecular weight of 1450 Da[2]. Vancomycin is a unique glycopeptide that is structurally unrelated to any currently available antibiotic. It also has a unique mode of action that inhibits the second phase of cell wall synthesis in susceptible bacteria. Vancomycin is active against a variety of Gram-positive bacteria, such as Staphylococcus aureus, Staph. epidermidis, Str. agalactiae, Str. bovis, Str. mutans, viridans streptococci, enterococci[3]. Vancomycin can be used in animal modeling to construct animal renal injury models. Vancomycin is administered intravenously with a standard infusion time of at least 1 hour to minimize infusion-related adverse reactions. In subjects with normal creatinine clearance, the α-distribution period of Vancomycin is 30 minutes to 1 hour, and the β-elimination half-life is 6-12 hours. The volume of distribution is 0.4–1 L/kg. Vancomycin is bound to proteins in the range of 10% to 50%. Factors that affect the overall activity of vancomycin include its tissue distribution, inoculum size, and protein binding effects [2]. Vancomycin treatment of infected mice was associated with improved clinical, diarrheal, and histopathological scores as well as survival during treatment [4]. Vancomycin is a classic renal injury modeling agent that induces disease by inducing oxidative stress-related cell apoptosis in animals. Rats and mice are commonly used as animal models [5][6]. Vancomycin induction dose reference [5][6]: (1) Model animal: C57BL/6J male mice (6 weeks) VIKI: 400 mg/kg/day, ip, 7 days (2) Model animal: male Sprague-Dawley (SD) rats (200-250g) VIKI: 400 mg/kg/day, ip, 7 days to induce renal injury model [5] Pathogenic mechanism Vancomycin induces disease by inducing oxidative stress-related cell apoptosis in animals. Specific modeling method Mice: C57BL/6 • male • 6-week-old Administration: 400 mg/kg • ip • once daily for 7 weeks Modeling success indicators Molecular changes: Induction of cell apoptosis and increased renal Cr, BUN, MDA, IL-1β, IL-6, TNF-α and NF-κB.
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References |
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Molecular Formula |
C70H67D10CL2F6N9O28
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Molecular Weight |
1687.36
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Appearance |
Typically exists as solid at room temperature
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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 | 0.5926 mL | 2.9632 mL | 5.9264 mL | |
5 mM | 0.1185 mL | 0.5926 mL | 1.1853 mL | |
10 mM | 0.0593 mL | 0.2963 mL | 0.5926 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.