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Description: Teicoplanin complex is an antibacterial agent used in the prophylaxis and treatment of serious infections caused by Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus and Enterococcus faecalis.
| ln Vitro |
In HEK293T cells, 2019nCoV-Spike virus in A549 cells, and SARS-CoV-2 virus in Vero E6 cells, tecoplanin sodium has antiviral action. The IC50 values are 0.39, 1.66, and 15.7 µM, respectively [1]. With an EC50 value of 17 µM, tecoplanin sodium suppresses the HIV-1 virus in human CEM cell cultures [1]. It works by interacting with the enzyme through the lipophilic portion of teicoplanin sodium. The anti-MRSA action of tecoplanin sodium is demonstrated by its MIC value of 0.5 mg/L against MRSA ATCC 43300 [2].
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|---|---|
| ln Vivo |
In a mouse model of MRSA infection, tecoplanin (10, 30 mg/kg; iv) showed dose-dependent decreases in total mushroom density [2].
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| Animal Protocol |
Animal/Disease Models: 20-30 g, male CD1 mice (2 * 106 cfu/ mL MRSA (43 300) 50 µL; mouse thigh infection model) [2]
Doses: 10, 30 mg/kg Route of Administration: intravenous (iv) (iv)injection ; Results every 12 hrs (hrs (hours)): It shows that the total bacterial density decreases in a dose-dependent manner, the dose ≥10 mg/kg/day can achieve the total bactericidal effect, and the dose ≥30 mg/kg/day can inhibit drug resistance. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Teicoplanin is not approved for marketing in the United States by the U.S. Food and Drug Administration, but is available in other countries. Limited data indicate that teicoplanin is poorly excreted into breastmilk. Because teicoplanin is not orally absorbed it is unlikely to adversely affect the breastfed infant. One infant was safely breastfed during maternal therapy with teicoplanin and ceftriaxone. Until more information becomes available, monitor the breastfed infant for gastrointestinal disturbances such as diarrhea, particularly in newborn and preterm infants. ◉ Effects in Breastfed Infants A mother who was exclusively nursing her 52-day-old infant developed a soft-tissue infection. She was treated with intravenous teicoplanin 400 mg every 12 hours for 3 doses, then 400 mg daily for 5 days total, intravenous ceftriaxone 1 gram daily, and topical mupirocin cream twice daily. A careful follow-up indicated that her infant had no adverse effects. |
| References | |
| Additional Infomation |
Teicoplanin has been reported in Streptomyces albidoflavus and Streptomyces coelicolor with data available.
Teicoplanin is a glycopeptide antibiotic complex isolated from the bacterium Actinoplanes teichomyceticus. Teicoplanin inhibits peptidoglycan polymerization, resulting in inhibition of bacterial cell wall synthesis and cell death. (NCI04) Lipoglycopeptide antibiotic from Actinoplanes teichomyceticus active against gram-positive bacteria. It consists of five major components each with a different fatty acid moiety. |
| Molecular Formula |
C88H97CL2N9O33
|
|---|---|
| Molecular Weight |
1879.6703
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| Exact Mass |
1877.556
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| CAS # |
61036-62-2
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| Related CAS # |
Teicoplanin sodium;184539-13-7
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| PubChem CID |
133065662
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| Appearance |
White to off-white solid powder
|
| Density |
1.7±0.1 g/cm3
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| Index of Refraction |
1.754
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| LogP |
0.4
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| Hydrogen Bond Donor Count |
24
|
| Hydrogen Bond Acceptor Count |
34
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| Rotatable Bond Count |
20
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| Heavy Atom Count |
132
|
| Complexity |
3920
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| Defined Atom Stereocenter Count |
22
|
| SMILES |
CCCCCCCCCC(=O)N[C@@H]1[C@H]([C@@H]([C@H](O[C@H]1OC2=C3C=C4C=C2OC5=C(C=C(C=C5)[C@H]([C@H]6C(=O)N[C@@H](C7=C(C(=CC(=C7)O)OC8[C@H]([C@H]([C@@H]([C@H](O8)CO)O)O)O)C9=C(C=CC(=C9)[C@H](C(=O)N6)NC(=O)[C@@H]4NC(=O)[C@@H]1C2=CC(=CC(=C2)OC2=C(C=CC(=C2)[C@H](C(=O)N[C@H](CC2=CC(=C(O3)C=C2)Cl)C(=O)N1)N)O)O)O)C(=O)O)O[C@H]1[C@@H]([C@H]([C@@H]([C@H](O1)CO)O)O)NC(=O)C)Cl)CO)O)O
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| InChi Key |
BJNLLBUOHPVGFT-CAYRISATSA-N
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| InChi Code |
InChI=1S/C88H97Cl2N9O33/c1-3-4-5-6-7-8-9-10-60(108)94-68-74(113)71(110)58(32-101)129-87(68)132-78-55-26-40-27-56(78)126-52-18-14-38(24-47(52)90)77(131-86-67(92-34(2)103)73(112)70(109)57(31-100)128-86)69-84(121)98-66(85(122)123)45-29-42(105)30-54(127-88-76(115)75(114)72(111)59(33-102)130-88)61(45)44-23-37(13-15-49(44)106)63(81(118)99-69)96-83(120)65(40)97-82(119)64-39-21-41(104)28-43(22-39)124-53-25-36(12-16-50(53)107)62(91)80(117)93-48(79(116)95-64)20-35-11-17-51(125-55)46(89)19-35/h11-19,21-30,48,57-59,62-77,86-88,100-102,104-107,109-115H,3-10,20,31-33,91H2,1-2H3,(H,92,103)(H,93,117)(H,94,108)(H,95,116)(H,96,120)(H,97,119)(H,98,121)(H,99,118)(H,122,123)/t48-,57-,58-,59-,62-,63-,64+,65-,66+,67-,68-,69+,70-,71-,72-,73-,74-,75+,76+,77-,86+,87+,88?/m1/s1
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| Chemical Name |
(1S,2R,19R,22R,34S,37R,40R,52S)-2-[(2R,3R,4R,5S,6R)-3-acetamido-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-22-amino-5,15-dichloro-64-[(2S,3R,4R,5S,6R)-3-(decanoylamino)-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-26,31,44,49-tetrahydroxy-21,35,38,54,56,59-hexaoxo-47-[(3S,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-7,13,28-trioxa-20,36,39,53,55,58-hexazaundecacyclo[38.14.2.23,6.214,17.219,34.18,12.123,27.129,33.141,45.010,37.046,51]hexahexaconta-3,5,8,10,12(64),14,16,23(61),24,26,29(60),30,32,41(57),42,44,46(51),47,49,62,65-henicosaene-52-carboxylic acid
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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 is not stable in solution, please use freshly prepared working solution for optimal results. |
| 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) |
H2O : ~100 mg/mL DMSO : ~25 mg/mL
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (Infinity 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 (Infinity 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 (Infinity 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: 120 mg/mL (Infinity 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 | 0.5320 mL | 2.6600 mL | 5.3201 mL | |
| 5 mM | 0.1064 mL | 0.5320 mL | 1.0640 mL | |
| 10 mM | 0.0532 mL | 0.2660 mL | 0.5320 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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