Apratastat

Modify Date: 2024-01-10 22:24:18

Apratastat Structure
Apratastat structure
Common Name Apratastat
CAS Number 287405-51-0 Molecular Weight 414.496
Density 1.4±0.1 g/cm3 Boiling Point N/A
Molecular Formula C17H22N2O6S2 Melting Point N/A
MSDS Chinese USA Flash Point N/A
Symbol GHS07
GHS07
Signal Word Warning

 Use of Apratastat


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].

 Names

Name Apratastat
Synonym More Synonyms

 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
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
GHS07
Signal Word Warning
Hazard Statements H302
Precautionary Statements P301 + P312 + P330
Hazard Codes Xi
RIDADR NONH for all modes of transport

 Articles2

More 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)

 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
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  • DC Chemicals Limited
  • China
  • Product Name: TMI-005
  • Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/500mg
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao


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