| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
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| ln Vitro |
Thiamphenicol was effective against β-lactamase-positive and Negative Haemophilus influenzae and demonstrated significant postantibiotic effects (PAE) (0.33 to 2.9 hours) against all pathogens studied (Streptococcus pneumoniae, Staphylococcus aureus, and Escherichia coli). The staphylococcus aureus and escherichia coli MICs were 32 mg/L, streptococcus pneumoniae was 2 mg/L, and hemophilus influenzae was 0.25 mg/L for the species under analysis. Thiamphenicol exhibits good in vitro action against multidrug-resistant bacteria that are challenging to treat [1].
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|---|---|
| ln Vivo |
The pharmacokinetics of thiamphenicol (30 mg/kg) following single intravenous (IV) and oral (PO) dosing were examined in Mulard ducks. After intravenous administration, the average residence time of thiamphenicol is 2.83 hours, the overall half-life is 1.96 hours, and the clearance rate is 0.04L/hr/kg. Pharmacokinetics following PO administration are essentially comparable to IV administration. Thiamphenicol is readily absorbed and its bioavailability surpasses 70% [2].
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| References | |
| Additional Infomation |
Thiamphenicol is a sulfone and a monocarboxylic acid amide. It has a role as an immunosuppressive agent and an antimicrobial agent.
A methylsulfonyl analog of CHLORAMPHENICOL. It is an antibiotic and immunosuppressive agent. |
| Molecular Formula |
C12H15CL2NO5S
|
|---|---|
| Molecular Weight |
356.2222
|
| Exact Mass |
355.004
|
| CAS # |
15318-45-3
|
| Related CAS # |
Thiamphenicol-d3;2211914-19-9;Thiamphenicol-d3-1;1217723-41-5
|
| PubChem CID |
27200
|
| Appearance |
White to off-white solid powder
|
| Density |
1.5±0.1 g/cm3
|
| Boiling Point |
695.9±55.0 °C at 760 mmHg
|
| Melting Point |
163-166ºC
|
| Flash Point |
374.7±31.5 °C
|
| Vapour Pressure |
0.0±2.3 mmHg at 25°C
|
| Index of Refraction |
1.583
|
| LogP |
-0.27
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
21
|
| Complexity |
443
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
CS(=O)(=O)C1=CC=C(C=C1)[C@H]([C@@H](CO)NC(=O)C(Cl)Cl)O
|
| InChi Key |
OTVAEFIXJLOWRX-NXEZZACHSA-N
|
| InChi Code |
InChI=1S/C12H15Cl2NO5S/c1-21(19,20)8-4-2-7(3-5-8)10(17)9(6-16)15-12(18)11(13)14/h2-5,9-11,16-17H,6H2,1H3,(H,15,18)/t9-,10-/m1/s1
|
| Chemical Name |
2,2-dichloro-N-[(1R,2R)-1,3-dihydroxy-1-(4-methylsulfonylphenyl)propan-2-yl]acetamide
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~280.73 mM)
H2O : ~2 mg/mL (~5.61 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.02 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 25.0 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: ≥ 2.5 mg/mL (7.02 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 25.0 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: ≥ 2.5 mg/mL (7.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8073 mL | 14.0363 mL | 28.0725 mL | |
| 5 mM | 0.5615 mL | 2.8073 mL | 5.6145 mL | |
| 10 mM | 0.2807 mL | 1.4036 mL | 2.8073 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00958503 | Completed | Drug: Thiamphenicol Drug: Placebo |
Healthy | Psyadon Pharma | 2007-07 | Phase 1 |
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