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Teicoplanin (Synonyms: Antibiotic 8327A, Antibiotic MDL 507, MDL 507)

Catalog No.GC11339 Copy One-Click Copy Product Info

Teicoplanin is a glycopeptide antibiotic of the vancomycin class obtained from fermentation by Actinoplanes teichomyceticus.

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Teicoplanin Chemical Structure

Cas No.: 61036-62-2

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50mg
$11.00
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100mg
$19.00
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500mg
$42.00
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1g
$60.00
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Sample solution is provided at 25 µL, 10mM.



Description of Teicoplanin

Teicoplanin is a glycopeptide antibiotic of the vancomycin class obtained from fermentation by Actinoplanes teichomyceticus. Teicoplanin binds to the D-Ala-D-Ala terminus of peptidoglycan precursors to block cell wall cross-linking and inhibit cell wall synthesis of Gram-positive bacteria, and enhances antibacterial effects through its hydrophobic side chain interfering with lipid II and cell membrane permeability. Teicoplanin can be used in research on infective endocarditis, osteomyelitis, septicemia caused by drug-resistant Gram-positive bacteria such as MRSA, and Clostridium difficile-associated diarrhea[1-4].

In vitro, Teicoplanin (1nM-100μM) treated Vero cells infected with EBOV Zaire GP/HIV core pseudovirus for 72h. Teicoplanin dose-dependently inhibited pEBOV infection with CC50>125μM[5]. Teicoplanin (130, 520, 890μg/mL) treated MCF-7 human breast cancer cells for 68h. Teicoplanin downregulated the mRNA expression of c-myc and c-fos in cells[6].

In vivo, Teicoplanin (1-120mg/kg; 4, 6, 8, 12, 24h intervals; 5 doses total) was intravenously administered 2h post-inoculation to cyclophosphamide-induced neutropenic mice with thigh Staphylococcus aureus infection (MSSA ATCC 29213 or MRSA ATCC 43300) for 24h treatment. Teicoplanin inhibited S. aureus burden growth in mouse thigh tissues[7]. Teicoplanin (100, 200, 500μg; single injection) was intracerebroventricularly injected (4μL/mouse; within 4min) into male ICR mice (5-6 weeks old; 25-30g). Teicoplanin induced behavioral seizures such as head twitching and forelimb clonus, accompanied by high-voltage polyspike waves in frontal cortex, hippocampus and amygdala[8].

References:
[1] Shea KW, Cunha BA. Teicoplanin. Med Clin North Am. 1995 Jul;79(4):833-44. doi: 10.1016/s0025-7125(16)30042-6.
[2] Parenti F, Schito GC, Courvalin P. Teicoplanin Chemistry and Microbiology. J Chemother. 2000 Nov;12 Suppl 5:5-14.
[3] Yushchuk O, Ostash B, Truman AW, et al. Teicoplanin biosynthesis: unraveling the interplay of structural, regulatory, and resistance genes. Appl Microbiol Biotechnol. 2020 Apr;104(8):3279-3291.
[4] Greenwood D. Microbiological properties of teicoplanin. J Antimicrob Chemother. 1988 Jan;21 Suppl A:1-13.
[5] Wang Y, Cui R, Li G, et al. Teicoplanin inhibits Ebola pseudovirus infection in cell culture. Antiviral Res. 2016 Jan;125:1-7.
[6] Ashouri S, Khujin MH, Kazemi M, et al. Effect of teicoplanin on the expression of c-myc and c-fos proto-oncogenes in MCF-7 breast cancer cell line. Adv Biomed Res. 2016 Nov 28;5:172.
[7] Watanabe E, Matsumoto K, Ikawa K, et al. Pharmacokinetic/pharmacodynamic evaluation of teicoplanin against Staphylococcus aureus in a murine thigh infection model. J Glob Antimicrob Resist. 2021 Mar;24:83-87.
[8] Takechi K, Ishikawa T, Kamei C. Epileptogenic activity induced by teicoplanin and effects of some antiepileptics in mice. J Pharmacol Sci. 2008 Aug;107(4):428-33.

Protocol of Teicoplanin

Cell experiment [1]:

Cell lines

MCF-7 cells (human breast cancer cell line)

Preparation Method

MCF-7 cells were maintained in RPMI-1640 medium supplemented with 100 units/mL penicillin G, 100μg/mL streptomycin and 10% fetal bovine serum at 37°C, 5% CO₂. MCF-7 cells were treated with Teicoplanin at 130, 520 and 890μg/mL for 68h, then harvested for MTT assay and real-time PCR to detect mRNA expression of c-myc and c-fos (normalized to GAPDH).

Reaction Conditions

130, 520, 890μg/mL; 68h

Applications

Teicoplanin treatment led to significant difference in MCF-7 cell proliferation rate compared with control groups. Teicoplanin significantly downregulated mRNA expression of c-myc and c-fos in MCF-7 cells at all three tested concentrations; the downregulation amplitude of c-myc at 890μg/mL was significantly lower than that at 130 and 520μg/mL, and the downregulation amplitude of c-fos at 520μg/mL was significantly stronger than that at 130μg/mL.
Animal experiment [2]:

Animal models

Neutropenic male ddY mice (5-week-old); thigh infection models were established by inoculating methicillin-susceptible Staphylococcus aureus (MSSA) ATCC 29213 or methicillin-resistant S. aureus (MRSA) ATCC 43300

Preparation Method

5-week-old male ddY mice were rendered neutropenic via intraperitoneal cyclophosphamide administration at 150mg/kg 4 days prior to infection and 100mg/kg 1 day prior to infection. For thigh infection model, 100μL early-log-phase S. aureus suspension (3.75×10⁶ CFU/mL) was intramuscularly injected into one posterior thigh muscle. Teicoplanin was administered intravenously 2h post-inoculation, with dosing regimens covering 1-120mg/kg at 4-, 6-, 8-, 12-, 24-h intervals (5 dose in total), mice were sacrificed 24h after initial dosing for thigh bacterial load enumeration via CFU counting.

Dosage form

1-120mg/kg; i.v.; 4/6/8/12/24h intervals; 5 dose in total

Applications

Teicoplanin dose-dependently inhibited S. aureus thigh burden growth in neutropenic mice.

References:
[1] Ashouri S, Khujin MH, Kazemi M, et al. Effect of teicoplanin on the expression of c-myc and c-fos proto-oncogenes in MCF-7 breast cancer cell line. Adv Biomed Res. 2016 Nov 28;5:172.
[2] Watanabe E, Matsumoto K, Ikawa K, et al. Pharmacokinetic/pharmacodynamic evaluation of teicoplanin against Staphylococcus aureus in a murine thigh infection model. J Glob Antimicrob Resist. 2021 Mar;24:83-87.

Chemical Properties of Teicoplanin

Cas No. 61036-62-2 SDF
Synonyms Antibiotic 8327A, Antibiotic MDL 507, MDL 507
Formula C77H77N9O31Cl2·R M.Wt 1564.3-1907.7
Solubility DMSO: 0.15 mg/ml,PBS (pH 7.2): 0.25 mg/ml Storage Store at 2-8°C,unstable in solution, ready to use.
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Teicoplanin

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 639.3 μL 3.1963 mL 6.3926 mL
5 mM 127.9 μL 639.3 μL 1.2785 mL
10 mM 63.9 μL 319.6 μL 639.3 μL
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In vivo Formulation Calculator (Clear solution) of Teicoplanin

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Product Documents of Teicoplanin

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Average Rating: 5 ★★★★★ (Based on Reviews and 23 reference(s) in Google Scholar.)

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