Apratastat

Names

[ Name ]:
Apratastat

[Synonym ]:
(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

Biological Activity

[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]:

Research Areas >> Cancer

Signaling Pathways >> Apoptosis >> TNF Receptor

Signaling Pathways >> Metabolic Enzyme/Protease >> MMP

[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.

Chemical & Physical Properties

[ 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

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ Precautionary Statements ]:
P301 + P312 + P330

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

Articles

ADAM17 mediates Nox4 expression and NADPH oxidase activity in the kidney cortex of OVE26 mice. Ford BM et al

Am. J. Physiol. Renal Physiol. 305(3) , F323-32, (2013)

Pharmacokinetic-pharmacodynamic modeling of apratastat: a population-based approach. Shu C et al

J. Clin. Pharmacol. 51(4) , 472-81, (2011)