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GW311616A . hydrochloride

AG-CR1-3632-M001 1 mg INQ
AG-CR1-3632-M005 5 mg INQ
AG-CR1-3632-M025 25 mg INQ
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Additional Information

Product Data
Synonyms (3S,3aS,6aR)-3-Isopropyl-1-(methylsulfonyl)-4-((E)-4-(piperidin-1-yl)but-2-enoyl)hexahydropyrrolo[3,2-b]pyrrol-2(1H)-one
Properties
Formula C19H31N3O4S . HCl
MW 397.5 . 36.5
CAS 197890-44-1
Purity ≥98% (NMR)
Appearance Solid.
Solubility Soluble in DMSO or water.
InChi Key UFCZUKYPBPXODT-OFTZGUNKSA-N
Product Type Chemical
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Keep cool and dry.
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
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Product Description

  • Potent, selective intracellular neutrophil elastase (NE, α-1-proteinase) inhibitor (by covalently binding to NE).
  • Inhibits human neutrophil elastase (HNE) and is selective over other human serine proteases with IC50 values of 22nM for HNE, >100μM for trypsin, cathepsin G and plasmin, >3μM for chymotrypsin and tissue plasminogen activator.
  • Specific β-cell proliferation promoter. Similar to SerpinB1, which functions through its inhibiting activity of several proteases including neutrophil elastase, cathepsin G and proteinase-3.
  • Reverses insulin resistance and body weight gain in HFD-fed mice, suggesting that the SerpinA1-NE system regulates AMPK signaling, fatty acid oxidation (FAO) and energy expenditure. The imbalance between SerpinA1 (α1-antitrypsin; A1AT) and neutrophil elastase NE contributes to the development of obesity and related inflammation, insulin resistance and liver steatosis.
  • Shown to inhibit tumor cell growth and proliferation and induce apoptosis in leukemia cell lines.

Product References

  1. The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase-GW311616A a development candidate: S.J. Macdonald, et al.; Bioorg. Med. Chem. Lett. 11, 895 (2001)
  2. Imbalance between neutrophil elastase and its inhibitor α1-antitrypsin in obesity alters insulin sensitivity, inflammation, and energy expenditure: V. Mansuy-Aubert, et al.; Cell Metab. 17, 534 (2013)
  3. Neutrophil elastase and its therapeutic effect on leukemia cells: K.L. Jiang, et al.; Mol. Med. Rep. 12, 4165 (2015)
  4. SerpinB1 Promotes Pancreatic β Cell Proliferation: A. El Ouaamari, et al.; Cell Metab. 23, 194 (2016)
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