| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 500mg |
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| 1g |
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| 5g | |||
| 10g | |||
| Other Sizes |
| Targets |
Chloramphenicol succinate sodium is a prodrug that is converted to the active drug, chloramphenicol. Chloramphenicol inhibits bacterial growth by inhibiting protein synthesis. It binds to the 50S ribosomal subunit and prevents peptide bond formation. The succinate prodrug form is inactive and requires hydrolysis to release the active chloramphenicol.
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|---|---|
| ln Vitro |
In vitro, Chloramphenicol succinate sodium itself is not active. Its activity is dependent on its conversion to chloramphenicol. The prodrug is typically tested for its stability and conversion rate in plasma or in the presence of esterases. The active drug, chloramphenicol, demonstrates broad-spectrum antibacterial activity.
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| ln Vivo |
In vivo, Chloramphenicol succinate sodium is administered parenterally. It is rapidly hydrolyzed to release the active chloramphenicol. This prodrug formulation allows for the administration of chloramphenicol to patients who cannot take oral medications. It is used to treat a number of bacterial infections.
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| Enzyme Assay |
For in vitro antibacterial susceptibility testing, the active drug, chloramphenicol, is tested. The prodrug, Chloramphenicol succinate sodium, is not typically tested directly. Standard procedures for determining the MIC against bacterial strains are followed. The prodrug's conversion can be studied in vitro using plasma or tissue homogenates.
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| Cell Assay |
For in vitro cell-based assays, the prodrug's conversion to chloramphenicol can be studied in cell culture. Its cytotoxicity to mammalian cells can be assessed.
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| Animal Protocol |
For in vivo animal studies, Chloramphenicol succinate sodium is administered parenterally. Its pharmacokinetics, including its conversion to chloramphenicol, are studied. Its efficacy in treating bacterial infections can be evaluated in animal models of infection.
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| ADME/Pharmacokinetics |
Chloramphenicol succinate sodium is administered parenterally. It is rapidly hydrolyzed to chloramphenicol. Chloramphenicol is metabolized in the liver and excreted in urine. The prodrug formulation has improved aqueous solubility.
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| Toxicity/Toxicokinetics |
Chloramphenicol succinate sodium can cause serious and potentially fatal side effects, including bone marrow suppression and aplastic anemia. It is used with caution and is typically reserved for serious infections where other antibiotics are ineffective. It is not intended for research use in humans.
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| References |
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| Additional Infomation |
According to state or federal labeling requirements, sodium chloramphenicol succinate may be carcinogenic. Sodium chloramphenicol succinate is a white powder. (NTP, 1992) Sodium chloramphenicol succinate is the sodium succinate salt of chloramphenicol, a nitrobenzene derivative and a broad-spectrum antibiotic with antibacterial activity. Sodium chloramphenicol succinate reversibly binds to the 50S subunit of bacterial ribosomes, thereby interfering with the activity of peptidyl transferases during protein synthesis elongation. Therefore, the drug inhibits bacterial cell growth. See also: Chloramphenicol (broad-spectrum).
Chloramphenicol succinate sodium is a clinically used antibiotic prodrug. It is available as an injectable formulation for parenteral administration. It is not typically used as a research compound, but it may be used as a reference standard. |
| Molecular Formula |
C₁₅H₁₅CL₂N₂NAO₈
|
|---|---|
| Molecular Weight |
445.18
|
| Exact Mass |
444.01
|
| Elemental Analysis |
C, 40.47; H, 3.40; Cl, 15.93; N, 6.29; Na, 5.16; O, 28.75
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| CAS # |
982-57-0
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| Related CAS # |
Chloramphenicol succinate;3544-94-3
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| PubChem CID |
656833
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| Appearance |
White to light yellow solid powder
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| Boiling Point |
716.3ºC at 760mmHg
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| Flash Point |
387ºC
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| LogP |
0.904
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
28
|
| Complexity |
541
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| Defined Atom Stereocenter Count |
2
|
| SMILES |
[Na+].OC(CCC(OC[C@H]([C@@H](C1=CC=C([N+]([O-])=O)C=C1)O)NC(C(Cl)Cl)=O)=O)=O
|
| InChi Key |
RPLOPBHEZLFENN-HTMVYDOJSA-M
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| InChi Code |
InChI=1S/C15H16Cl2N2O8.Na/c16-14(17)15(24)18-10(7-27-12(22)6-5-11(20)21)13(23)8-1-3-9(4-2-8)19(25)26/h1-4,10,13-14,23H,5-7H2,(H,18,24)(H,20,21)/q+1/p-1/t10-,13-/m1./s1
|
| Chemical Name |
sodium 4-((2R,3R)-2-(2,2-dichloroacetamido)-3-hydroxy-3-(4-nitrophenyl)propoxy)-4-oxobutanoate
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| Synonyms |
Chloramphenicol sodium succinate; CCRIS6204; CCRIS-6204; CCRIS 6204
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~125 mg/mL (~280.79 mM)
H2O : ~50 mg/mL (~112.31 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.67 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.67 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (224.63 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2463 mL | 11.2314 mL | 22.4628 mL | |
| 5 mM | 0.4493 mL | 2.2463 mL | 4.4926 mL | |
| 10 mM | 0.2246 mL | 1.1231 mL | 2.2463 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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