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Chemical Structure| 168828-58-8 Chemical Structure| 168828-58-8

Structure of Sutezolid
CAS No.: 168828-58-8

Chemical Structure| 168828-58-8

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Sutezolid (PNU-100480) is an orally active oxazolidinone antibiotic that works by inhibiting bacterial protein synthesis. Sutezolid has strong antimycobacterial activity and is used in research on drug-resistant tuberculosis.

Synonyms: PNU-100480; U-100480; PF-02341272

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Product Details of Sutezolid

CAS No. :168828-58-8
Formula : C16H20FN3O3S
M.W : 353.41
SMILES Code : O=C(O[C@H]1CNC(C)=O)N(C1)C2=CC(F)=C(N3CCSCC3)C=C2
Synonyms :
PNU-100480; U-100480; PF-02341272
MDL No. :MFCD00937821

Safety of Sutezolid

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Nonreplicating Mycobacterium tuberculosis 1 μg/ml 28 to 35 days To evaluate the bactericidal effect of Sutezolid against dormant Mycobacterium tuberculosis under conditions mimicking caseous granulomas (hypoxia at neutral pH). Results showed that Sutezolid alone had limited efficacy but was effective in combination with rifampin-nitazoxanide in killing dormant cells. Antimicrob Agents Chemother. 2019 Jun 24;63(7):e00273-19
Nonreplicating SS18b cells 2.5 μg/ml 7 days Evaluate the bactericidal effect of Sutezolid on nonreplicating Mycobacterium tuberculosis, results showed Sutezolid has strong bactericidal activity. Antimicrob Agents Chemother. 2014 Jun;58(6):3217-23
Mycobacterium tuberculosis H37Rv 2.5 μg/ml 7 days Evaluate the bacteriostatic effect of Sutezolid on actively growing Mycobacterium tuberculosis, results showed Sutezolid has bacteriostatic activity. Antimicrob Agents Chemother. 2014 Jun;58(6):3217-23
Mycobacterium tuberculosis H37Rv 0.20 μg/ml 7 days Evaluate the bactericidal activity of STZ alone and in combination with MCZ. STZ alone showed no dose-dependent bactericidal activity, but in combination with MCZ at their respective MICs, it significantly reduced bacterial burden (2 log10 CFU/ml). Antimicrob Agents Chemother. 2018 Oct 24;62(11):e00840-18

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c mice Nonreplicating Mycobacterium tuberculosis 18b infection model Oral 100 mg/kg Five times a week for 4 weeks Evaluate the bactericidal effect of Sutezolid on nonreplicating Mycobacterium tuberculosis in vivo, results showed Sutezolid exhibited significant bactericidal activity in both lungs and spleens. Antimicrob Agents Chemother. 2014 Jun;58(6):3217-23
BALB/c mice TB infection model Oral gavage 100 mg/kg 5 days/week for 4 weeks Evaluate the in vivo efficacy of STZ combined with MCZ and DMD. Although no synergism was observed, the triple combination (MCZ-DMD-STZ) showed superior bactericidal activity in lungs compared to the RHZ standard regimen (1.17 log10 CFU reduction). Antimicrob Agents Chemother. 2018 Oct 24;62(11):e00840-18
CD-1 mice Murine model of tuberculosis Oral gavage 25, 50, 100 mg/kg 5 days per week for 4 weeks Evaluate the efficacy of Sutezolid in a murine tuberculosis model, showing comparable activity to isoniazid at 100 mg/kg Antimicrob Agents Chemother. 1999 May;43(5):1189-91
BALB/c mice TB infection model Oral gavage 50 mg/kg 5 days per week for 4, 6, or 8 weeks To evaluate the bactericidal and sterilizing activity of sutezolid in combination with S587 and pretomanid, showing superior activity to linezolid in preventing relapse. Antimicrob Agents Chemother. 2023 Apr 18;67(4):e0003523
Mice Murine model of tuberculosis Oral 50 mg/kg 5 days per week for 8 weeks To evaluate the bactericidal and sterilizing activities of Sutezolid in combination with other drugs against tuberculosis, results showed that TMC207 plus PNU-100480 was the most effective drug pair. Antimicrob Agents Chemother. 2012 Jun;56(6):3114-20

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.83mL

0.57mL

0.28mL

14.15mL

2.83mL

1.41mL

28.30mL

5.66mL

2.83mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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