Sutezolid - CAS 168828-58-8
Catalog number: B0084-458614
Category: Inhibitor
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Molecular Formula:
C16H20FN3O3S
Molecular Weight:
353.41
COA:
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Targets:
Antibacterial
Description:
Sutezolid, also called as PNU-100480, is an oxazolidinone antibacterial compound to reach Phase-II clinical research for Tuberculosis.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-458614 25 mg $199 In stock
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Purity:
95%
Appearance:
Solid powder
Synonyms:
N-[[(5S)-3-(3-fluoro-4-thiomorpholin-4-ylphenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamidePF-02341272; PF02341272; PF 02341272; PNU-100480; PNU 100480; PNU100480; U-100480; U 100480; U100480; Sutezolid.168828-58-8
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -74℃ for long term (months to years).
MSDS:
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Shelf Life:
2 years
Quantity:
Grams-Kilos
Boiling Point:
609ºC at 760 mmHg
Density:
1.321g/cm3
InChIKey:
FNDDDNOJWPQCBZ-ZDUSSCGKSA-N
InChI:
1S/C16H20FN3O3S/c1-11(21)18-9-13-10-20(16(22)23-13)12-2-3-15(14(17)8-12)19-4-6-24-7-5-19/h2-3,8,13H,4-7,9-10H2,1H3,(H,18,21)/t13-/m0/s1
Canonical SMILES:
CC(=O)NCC1CN(C(=O)O1)C2=CC(=C(C=C2)N3CCSCC3)F
1.Population pharmacokinetic/pharmacodynamic analysis of the bactericidal activities of sutezolid (PNU-100480) and its major metabolite against intracellular Mycobacterium tuberculosis in ex vivo whole-blood cultures of patients with pulmonary tuberculosis.
Zhu T1, Friedrich SO2, Diacon A2, Wallis RS3. Antimicrob Agents Chemother. 2014 Jun;58(6):3306-11. doi: 10.1128/AAC.01920-13. Epub 2014 Mar 31.
Sutezolid (PNU-100480 [U-480]) is an oxazolidinone antimicrobial being developed for the treatment of tuberculosis. An active sulfoxide metabolite (PNU-101603 [U-603]), which reaches concentrations in plasma several times those of the parent, has been reported to drive the killing of extracellular Mycobacterium tuberculosis by sutezolid in hollow-fiber culture. However, the relative contributions of the parent and metabolite against intracellular M. tuberculosis in vivo are not fully understood. The relationships between the plasma concentrations of U-480 and U-603 and intracellular whole-blood bactericidal activity (WBA) in ex vivo cultures were examined using a direct competitive population pharmacokinetic (PK)/pharmacodynamic 4-parameter sigmoid model. The data set included 690 PK determinations and 345 WBA determinations from 50 tuberculosis patients enrolled in a phase 2a sutezolid trial. The model parameters were solved iteratively.
2.Mycobactericidal activity of sutezolid (PNU-100480) in sputum (EBA) and blood (WBA) of patients with pulmonary tuberculosis.
Wallis RS1, Dawson R2, Friedrich SO3, Venter A4, Paige D5, Zhu T5, Silvia A5, Gobey J5, Ellery C5, Zhang Y5, Eisenach K6, Miller P1, Diacon AH3. PLoS One. 2014 Apr 14;9(4):e94462. doi: 10.1371/journal.pone.0094462. eCollection 2014.
RATIONALE: Sutezolid (PNU-100480) is a linezolid analog with superior bactericidal activity against Mycobacterium tuberculosis in the hollow fiber, whole blood and mouse models. Like linezolid, it is unaffected by mutations conferring resistance to standard TB drugs. This study of sutezolid is its first in tuberculosis patients.
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CAS 168828-58-8 Sutezolid

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