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Tedizolid (Synonyms: DA 7157, TR-700)

Katalog-Nr.GC13891

An oxazolidinone antibiotic

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Tedizolid Chemische Struktur

Cas No.: 856866-72-3

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10mM (in 1mL DMSO)
77,00 $
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5mg
69,00 $
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10mg
123,00 $
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50mg
357,00 $
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

Protocol

Cell experiment [1]:

Cell lines

PRSP (penicillin G MICs≥2 μg/ml) clinical isolates

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

20h; MIC90=0.25 μM

Applications

Agar dilution experiments demonstrated that all 28 clinical isolates of PRSP were inhibited by tedizolid at 0.25 μg/ml (MIC range, 0.125 to 0.25 μg/ml) and all were inhibited by linezolid at 1μg/ml (MIC range, 0.125 to 1 μg/ml). Tedizolid was 4-fold more potent than linezolid against PRSP; MIC90s were 0.25 μg/ml with tedizolid and 1 μg/ml with linezolid.

Animal experiment [1]:

Animal models

Male ICR mice

Dosage form

10 mg/kg (QD); intraperitoneal inoculation

Applications

The majority (80%) of the untreated control mice infected with PSSP type III succumbed to the infection within 7 days. For infected mice receiving 48 h treatment with tedizolid phosphate at 2.5 mg/kg QD and 5 mg/kg QD (total daily doses, 2.5 mg/kg and 5 mg/kg, respectively), the 15-day cumulative survival rates were 50% and 80%, respectively. A 100% survival rate was achieved with tedizolid phosphate at a minimum total daily dose of 10 mg/kg (QD), which was 4-fold lower than the 40-mg/kg total daily dose of linezolid (BID) needed to obtain 100% survival. On the basis of the ED50 values in the murine pneumococcal pneumonia model, tedizolid phosphate was nearly 3-fold more potent than linezolid, with ED50s of 2.80 mg/kg/day (95% CI, 1.41 to 4.44) versus 8.09 mg/kg/day (95% CI, 4.74 to 11.91)

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Choi S, Im W, Bartizal K. Activity of Tedizolid Phosphate (TR-701) in murine models of infection with penicillin-resistant and penicillin-sensitive streptococcus pneumoniae[J]. Antimicrobial agents and chemotherapy, 2012, 56(9): 4713-4717.

Background

Tedizolid is an oxazolidinone antimicrobial agent with MIC50 value of 0.5 μg/ml for MSSA, MRSA, VR E. faecium and VR E. faecalis and 0.25 μg/ml for MSSE, MRSE, PSSP and PRSP [1].

The resistant Gram-positive infection is a serious global health problem. For instant, the methicillin-resistant S. aureus (MRSA) has spread all over the world with rates ranging from 18 to 26 cases among 100,000 people. Besides that, there come out a serious of resistant strains such as the linezolid-resistant S. aureus (LRSA) and the vancomycin-resistant S. aureus (VRSA). Due to the unfavorable outcomes of the existed antibiotics, alternative treatments have been developed. Tedizolid is a synthetic antibiotic that works based on the inhibition of protein synthesis. It binds to the 50S ribosome and inhibits the formation of the 70S complex [1].

Tedizolid showed potent bacteriostatic activity against many resistant Gram-positive pathogens such as MSSA, MRSA, S. pyogenes and S. pneumoniae. For the enterococcal and staphylococcal isolates, tedizolid displayed more than 4-fold higher potency than that of linezolid. It also showed inhibitory effects on a panel of 169 linezolid-resistant staphylococcal isolates with 79.2% inhibition at concentration of ≤ 4μg/ml. The MIC values of tedizolid against linezolid-resistant staphylococci were in a range from 0.06 to 16 mg/L. Besides that, tedizolid was found to be the inhibitors of human monoamine oxidase with IC50 values of 8.7 and 5.7 μM for MAO-A and MAO-B, respectively [1, 2 and 3].

When treated in vivo, tedizolid was the active moiety converted from the pro-drug tedizolid phosphate. It was found that granulocytes could affect the antistaphylococcal effect of tedizolid. In neutropenic mice, the administration of tedizolid for 24 hours or 48 hours caused ED50 values of 25.2 and 35.7 mg/kg/day, respectively [1 and 4].

References:
[1] Kanafani Z A, Corey G R.  Tedizolid (TR-701): a new oxazolidinone with enhanced potency. Expert opinion on investigational drugs, 2012, 21(4): 515-522.
[2] Rodríguez-Avial I, Culebras E, Betriu C, et al.  In vitro activity of tedizolid (TR-700) against linezolid-resistant staphylococci. Journal of antimicrobial chemotherapy, 2012, 67(1): 167-169.
[3] Flanagan S, Bartizal K, Minassian S L, et al.  In vitro, in vivo, and clinical studies of tedizolid to assess the potential for peripheral or central monoamine oxidase interactions. Antimicrobial agents and chemotherapy, 2013, 57(7): 3060-3066.
[4] Louie A, Liu W, Kulawy R, et al.  In vivo pharmacodynamics of torezolid phosphate (TR-701), a new oxazolidinone antibiotic, against methicillin-susceptible and methicillin-resistant Staphylococcus aureus strains in a mouse thigh infection model. Antimicrobial agents and chemotherapy, 2011, 55(7): 3453-3460.

Chemical Properties

Cas No. 856866-72-3 SDF
Überlieferungen DA 7157, TR-700
Chemical Name (5R)-3-[3-fluoro-4-[6-(2-methyltetrazol-5-yl)pyridin-3-yl]phenyl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one
Canonical SMILES CN1N=C(N=N1)C2=NC=C(C=C2)C3=C(C=C(C=C3)N4CC(OC4=O)CO)F
Formula C17H15FN6O3 M.Wt 370.34
Löslichkeit ≥ 9.25 mg/mL in DMSO with gentle warming Storage Store at -20°C
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

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.7002 mL 13.5011 mL 27.0022 mL
5 mM 0.54 mL 2.7002 mL 5.4004 mL
10 mM 0.27 mL 1.3501 mL 2.7002 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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