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287405-51-0

287405-51-0 structure
287405-51-0 structure
  • Name: Apratastat
  • Chemical Name: Apratastat
  • CAS Number: 287405-51-0
  • Molecular Formula: C17H22N2O6S2
  • Molecular Weight: 414.496
  • Catalog: Signaling Pathways Apoptosis TNF Receptor
  • Create Date: 2018-06-03 20:30:05
  • Modify Date: 2025-08-24 22:29:16
  • Apratastat is an orally active, potent, and reversible dual inhibitor of tumor necrosis factor-α converting enzyme (TACE) and matrix metalloproteinases (MMPs) . Apratastat can potently inhibit the release of TNF-α in vitro, ex vivo, and in vivo with IC50s of 144 ng/mL in vitro and 81.7 ng/mL ex vivo, respectively[1].

Name Apratastat
Synonyms (3S)-N-Hydroxy-4-({4-[(4-hydroxy-2-butyn-1-yl)oxy]phenyl}sulfonyl)-2,2-dimethyl-3-thiomorpholinecarboxamide
TMI 005
(3S)-N-hydroxy-4-({4-[(4-hydroxybut-2-yn-1-yl)oxy]phenyl}sulfonyl)-2,2-dimethylthiomorpholine-3-carboxamide
MFCD13152357
3-Thiomorpholinecarboxamide, N-hydroxy-4-[[4-[(4-hydroxy-2-butyn-1-yl)oxy]phenyl]sulfonyl]-2,2-dimethyl-, (3S)-
Apratastat
Description Apratastat is an orally active, potent, and reversible dual inhibitor of tumor necrosis factor-α converting enzyme (TACE) and matrix metalloproteinases (MMPs) . Apratastat can potently inhibit the release of TNF-α in vitro, ex vivo, and in vivo with IC50s of 144 ng/mL in vitro and 81.7 ng/mL ex vivo, respectively[1].
Related Catalog
Target

TNF-α

MMP

References

[1]. Shu C, et al. Pharmacokinetic-pharmacodynamic modeling of apratastat: a population-based approach. J Clin Pharmacol. 2011 Apr;51(4):472-81.

Density 1.4±0.1 g/cm3
Molecular Formula C17H22N2O6S2
Molecular Weight 414.496
Exact Mass 414.091919
LogP 1.42
Index of Refraction 1.607
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Precautionary Statements P301 + P312 + P330
Hazard Codes Xi
RIDADR NONH for all modes of transport
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