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Elastase

Elastase is a serine protease that catalyzes not only the hydrolysis of peptide bonds of proteins but also the hydrolysis of amides and esters. Although it has similar functions as trypsin and chymotrypsin, elastase preferentially targets the protein elastin catalyzing cleavage at its neutral sites. Two major types of elastase have been identified, including pancreatic elastase and neutrophil elastase (PMN). While he pancreatic elastase is produced initially as an inactive protein requiring the activation by trypsin in the duodenum; PMN is found in relatively high levels in the azurophilic granules of circulating leukocytes and neutrophils. Both types of elastase exhibit similar activities but differ in substrate specificity and inhibitor profile.

  1. Cat.No. Product Name Information
  2. B1037 Alvelestat Alvelestat is an orally bioavailable inhibitor of neutrophil elastase (NE) with IC50 value of pIC50 value of 7.9 .
  3. A4432 ARP 100 ARP 100 is a selective inhibitor of matrix metalloproteinases 2 (MMP-2) with IC50 value of 12 nM [1].
  4. C4325 BAY-678
  5. C3609 (Z-Ala-Ala-Ala-Ala)2Rh110
  6. C3252 Neutrophil Elastase Inhibitor
  7. B6189 Sivelestat (ONO-5046)
  8. A4431 SSR 69071 High affinity, potent inhibitor of human leukocyte elastase (HLE) (IC50 = 3.9 nM). Displays species-selectivity (Ki values are 0.017, 1.70, 3.01, 58 and > 100 nM?for human, mouse, rat, rabbit and porcine elastase respectively). Inhibits HLE-induced lung hemorrhage in mice (ID50 = 2.8 mg/kg) and reduces infarct size in an in vivo acute model of coronary ischemia-reperfusion injury. Orally active.
  9. A4430 Sivelestat sodium salt Selective leukocyte elastase inhibitor (IC50 = 44 nM) that displays no activity at a range of other proteases. Inhibits NF-κB activation and LTB4-induced neutrophil transmigration in vitro. Significantly attenuates ischemia-induced spinal cord injury, decreases serum cytokine levels and reduces acute inflammatory lung injury in vivo.
  10. B4676 GW311616 hydrochloride GW311616 hydrochloride is a potent, selective, intracellular, orally bioavailable and long duration inhibitor of human neutrophil elastase (HNE) with an IC50 value of 22nM .
  11. B4675 GW311616

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