Size | Price | Stock | Qty |
---|---|---|---|
1g |
|
||
Other Sizes |
|
Purity: ≥98%
Sultamicillin Tosylate, the tosylate salt form of Sultamicillin which is a double ester of sulbactam and ampicillin. Sultamicillin (formerly known as CP-49952 and VD 1827) is an orally available, mutual prodrug form of ampicillin and sulbactam. As an antibiotic combination (co-drug or mutual prodrug) of ampicillin/sulbactam, it contains esterified ampicillin and sulbactam and is marketed under a number of trade names, e. g. Unasyn from Pfizer. Ampicillin is a semi-synthetic orally active broad spectrum antibiotic which is linked via a methylene group with a beta-lactamase inhibitor. Sultamicillin is chemically oxymethyl penicillinate sulfone ester of ampicillin. After absorption, sultamicillin releases ampicillin and sulbactam into the system, so all the antibacterial efficacy of sultamicillin is due to ampicillin and sulbactam. Ampicillin exerts antibacterial activity against sensitive organisms by inhibiting biosynthesis of cell wall mucopeptide where as sulbactam irreversibly inhibits most important beta-lactamases that occur in resistant strains.
Targets |
β-lactam
|
||
---|---|---|---|
ln Vitro |
Sultamicillin tosylate shows antibacterial activity against MRSA with a MIC value of 25 μg/mL[4].
|
||
ln Vivo |
Sultamicillin tosylate is hydrolyzed to yield Sulbactam (HY-B0334) and Ampicillin (HY-B0522) after oral absorption[2].
When combined with an immunosuppressive medication (such as mycophenolate mofetil (HY-B0199) and methylprednisolone (HY-B0260), streptomycin (oral gavage, every 12 hours) significantly increases the survival of experimental polymicrobial sepsis in mice and improves bacterial clearance[3]. |
||
Animal Protocol |
|
||
References |
|
Molecular Formula |
C32H38N4O12S3
|
---|---|
Molecular Weight |
766.86
|
Elemental Analysis |
C, 47.87; H, 5.27; N, 6.98; O, 27.90; S, 11.98
|
CAS # |
83105-70-8
|
Related CAS # |
76203-99-1 (HCl);76497-13-7 (free);83105-70-8;
|
Appearance |
Solid powder
|
SMILES |
O=S(C1=CC=C(C)C=C1)(O)=O.O=C([C@@H](C(C)(C)S([C@]2([H])C3)(=O)=O)N2C3=O)OCOC([C@@H](C(C)(C)S[C@]4([H])[C@@H]5NC([C@H](N)C6=CC=CC=C6)=O)N4C5=O)=O.[H]O[H].[H]O[H]
|
InChi Key |
KNVDAMRBJYZXRW-ZAKZIJIGSA-N
|
InChi Code |
InChI=1S/C25H30N4O9S2.C7H8O3S/c1-24(2)17(29-20(32)16(21(29)39-24)27-19(31)15(26)12-8-6-5-7-9-12)22(33)37-11-38-23(34)18-25(3,4)40(35,36)14-10-13(30)28(14)18;1-6-2-4-7(5-3-6)11(8,9)10/h5-9,14-18,21H,10-11,26H2,1-4H3,(H,27,31);2-5H,1H3,(H,8,9,10)/t14-,15-,16-,17+,18+,21-;/m1./s1
|
Chemical Name |
[(2S,5R)-3,3-dimethyl-4,4,7-trioxo-4lambda6-thia-1-azabicyclo[3.2.0]heptane-2-carbonyl]oxymethyl (2S,5R,6R)-6-[[(2R)-2-amino-2-phenylacetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate;4-methylbenzenesulfonic acid
|
Synonyms |
Sultamicillin tosilate; Sultamicillin tosylate hydrate; Sultamicillin; CP-49,952; CP 49,952; CP49,952; CP-49952; CP 49952; CP49952. VD 1827; Bacimex; p-Toluenesulfonate Sbtpc; Unacid PD oral; acim orale.
|
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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
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 : 100~125 mg/mL ( 130.4~163.00 mM )
Ethanol : ~100 mg/mL Water : ~9 mg/mL |
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.71 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 (2.71 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 (2.71 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: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.08 mg/mL (2.71 mM) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.3040 mL | 6.5201 mL | 13.0402 mL | |
5 mM | 0.2608 mL | 1.3040 mL | 2.6080 mL | |
10 mM | 0.1304 mL | 0.6520 mL | 1.3040 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.