Elastase-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Elastase.html ElastaseElastase is a group of serine proteases that include the macrophage elastase, the fibroblast elastase, the neutrophil elastase, andthe pancreatic elastase. Elastase can not only cleave the important connective tissue protein elastin, but a

2、lso facilitate thedegradation of the extracellular matrix such as fibronectin; laminin; collagens III, IV, and VI; and proteoglycans.Mammalian elastases occur mainly in the pancreas and the phagocytes. Among non-mammalian elastases there is a great variety ofbacterial metallo and serine elastases. T

3、he elastolytic activity varies from one elastase to another and is usually not correlated withthe catalytic efficiency of these proteinases. There is a large number of natural (proteins) and synthetic elastase inhibitors. Elastasesplay a pathologic role in pulmonary emphysema, cystic fibrosis, infec

4、tions, inflammation, and atherosclerosis.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Elastase.html Elastase HYPERLINK https:/www.MedChemE/Targets/Elastase.html HYPERLINK https:/www.MedChemE/Targets/Elastase.html Inhibitors HYPERLINK https:/www.MedChemE/19-hydroxyasiatic-acid.html 19-Hydroxy

5、asiatic HYPERLINK https:/www.MedChemE/19-hydroxyasiatic-acid.html HYPERLINK https:/www.MedChemE/19-hydroxyasiatic-acid.html acid HYPERLINK https:/www.MedChemE/19-hydroxyasiatic-acid.html HYPERLINK https:/www.MedChemE/AE-3763.html AE-3763Cat. No.: HY-N8164 Cat. No.: HY-1940619-Hydroxyasiatic acid, a

6、natural triterpenoid,possesses anti-elastase activity.AE-3763 is a peptide-based human neutrophilelastase inhibitor with an IC of 29 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChe

7、mE/Alvelestat.html Alvelestat(AZD9668) Cat. No.: HY-15651 HYPERLINK https:/www.MedChemE/alvelestat-tosylate.html Alvelestat HYPERLINK https:/www.MedChemE/alvelestat-tosylate.html HYPERLINK https:/www.MedChemE/alvelestat-tosylate.html tosylate(AZD9668 tosylate) Cat. No.: HY-15651AAlvelestat (AZD9668)

8、 is an orally bioavailable,affinity and selective inhibitor of neutrophilelastase (NE) pICwith a 50 value of 7.9 nM, a Kivalue of 9.4 nM and a K value of 9.5 nM.dAlvelestat (tosylate) is an orally bioavailable,affinity and selective inhibitor of neutrophilelastase (NE) with a pIC value of 7.9 nM, a5

9、0 Kivalue of 9.4 nM and a K value of 9.5 nM.dPurity: 99.27%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/BAY-678.html BAY-678 HYPERLINK https:/www.MedChemE/BAY-678.html HYPERLINK https

10、:/www.MedChemE/BAY-678_racemate.html BAY-678 HYPERLINK https:/www.MedChemE/BAY-678_racemate.html HYPERLINK https:/www.MedChemE/BAY-678_racemate.html racemateCat. No.: HY-111457A Cat. No.: HY-111515BAY-678 is an orally bioavailable, highly potent,selective and cell-permeable inhibitor of humanneutrop

11、hil elastase (HNE), with an IC of 20 nM.50BAY-678 is also nominated as a chemical probe tothe public via the Structural Genomics Consortium(SGC).BAY-678 racemate is a racemate of BAY-678. BAY-678is an orally bioavailable, highly potent,selective and cell-permeable inhibitor of humanneutrophil elasta

12、se (HNE), with an IC of 20 nM.50Purity: 99.24%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/BAY-85-8501.html BAY-85-8501 HYPERLINK https:/www.MedChemE/BAY-85-850

13、1.html HYPERLINK https:/www.MedChemE/chrysophanol-8-o-glucoside.html Chrysophanol HYPERLINK https:/www.MedChemE/chrysophanol-8-o-glucoside.html HYPERLINK https:/www.MedChemE/chrysophanol-8-o-glucoside.html 8-O-glucosideCat. No.: HY-19908 Cat. No.: HY-N2395BAY-85-8501 is a selective, reversible and p

14、otentinhibitor of Human Neutrophil Elastase (HNE),with an IC of 65 pM.50Chrysophanol 8-O-glucoside, from the roots ofRumex acetosa, shows moderate elastase inhibitionactivity.Purity: 99.24%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Da

15、ta: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/cyclotheonellazole-a.html Cyclotheonellazole HYPERLINK https:/www.MedChemE/cyclotheonellazole-a.html HYPERLINK https:/www.MedChemE/cyclotheonellazole-a.html A HYPERLINK https:/www.MedChemE/cyclotheonellazole-a.html HYPERLINK

16、https:/www.MedChemE/DMP-777.html DMP HYPERLINK https:/www.MedChemE/DMP-777.html HYPERLINK https:/www.MedChemE/DMP-777.html 777Cat. No.: HY-P3356(L-694458) Cat. No.: HY-75957Cyclotheonellazole A is a natural macrocyclicpeptide and a potent elastase inhibitor (IC =0.03450nM). Cyclotheonellazole A inhi

17、bits chymotrypsinwith an IC value of 0.62 nM.50DMP 777 is a potent, selective, and orally activehuman leukocyte elastase (HLE) inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.13%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 1

18、00 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/elastatinal.html Elastatinal HYPERLINK https:/www.MedChemE/elastatinal.html HYPERLINK https:/www.MedChemE/fk706.html FK706Cat. No.: HY-100397 Cat. No.: HY-19269Elastatinal is a potent and competitive inhibi

19、torof elastase, with a K of 0.21 M. Elastatinal moreipotently inhibits pancreatic elastase versusleucocyte elastase. Elastatinal shows no activityon human leucocyte chymotrypsin-like protease.FK706 is a potent, slow-binding and competitiveinhibitor of human neutrophil elastase with anIC of 83 nM and

20、 a of 4.2 nM.50 KiPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.57%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/freselestat.html Freselestat(ONO-6818; ONO-PO-736) Cat. No.: HY-15652 HYPERLINK https:/www.MedChemE/freselesta

21、t-quarterhydrate.html Freselestat HYPERLINK https:/www.MedChemE/freselestat-quarterhydrate.html HYPERLINK https:/www.MedChemE/freselestat-quarterhydrate.html quarterhydrate(ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate) Cat. No.: HY-15652AFreselestat (ONO-6818) is a potent and orallyactive neut

22、rophil elastase inhibitor with a K ofi12.2 nM.Freselestat quarterhydrate (ONO-6818quarterhydrate) is a potent and orally activeneutrophil elastase inhibitor with a K of 12.2 nM.iPurity: 98%Clinical Data: No Development ReportedSize: 10 mgPurity: 99.0%Clinical Data: No Development ReportedSize: 5 mg

23、HYPERLINK https:/www.MedChemE/GW311616.html GW311616Cat. No.: HY-15891 HYPERLINK https:/www.MedChemE/gw311616-hydrochloride.html GW311616 HYPERLINK https:/www.MedChemE/gw311616-hydrochloride.html HYPERLINK https:/www.MedChemE/gw311616-hydrochloride.html hydrochloride(GW311616A) Cat. No.: HY-15891AGW

24、-311616 is a potent, orally bioavailable, longduration and selective human neutrophil elastase(HNE) inhibitor with IC value of 22 nM and50 Kivalue of 0.31 nM.GW-311616 is a potent, orally bioavailable, longduration and selective human neutrophil elastase(HNE) inhibitor with IC50 value of 22 nM and K

25、ivalue of 0.31 nM.Purity: 99.52%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mgPurity: 98.84%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/jcp174.html JCP174 HYPERLINK https:/www.MedChemE/jcp174.html HYPERLINK https:/www.MedChemE/Lodelaben.html Lo

26、delabenCat. No.: HY-118621(SC-39026; Declaben) Cat. No.: HY-100240JCP174 is an inhibitor of palmitoyl proteinthioesterase-1 (TgPPT1), a depalmitoylase in theparasite T. gondii. JCP174 is also an inhibitor ofporcine pancreatic elastase and human leukocyteelastase.Lodelaben is a human neutrophil elast

27、ase inhibitorwith an IC50 and Ki of 0.5 and 1.5 M,respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 95.0%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/lonodelestat.html Lonodelestat HYPERLINK https:/www.MedChemE/lonodelestat.html H

28、YPERLINK https:/www.MedChemE/secologanoside.html Secologanoside(POL6014) Cat. No.: HY-P3293Cat. No.: HY-N6876Lonodelestat (POL6014) is a potent, orally activeand selective peptide inhibitor of humanneutrophil elastase (hNE).Secologanoside is a triterpenoid isolated fromPoraqueiba sericea, weakly inh

29、ibits elastase with anIC of 164 g/mL. Secologanoside is moderate50cytotoxic to fibroblasts.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/sivelestat.html Sivelestat(EI546;

30、 LY544349; ONO5046) Cat. No.: HY-17443 HYPERLINK https:/www.MedChemE/Sivelestat-sodium.html Sivelestat HYPERLINK https:/www.MedChemE/Sivelestat-sodium.html HYPERLINK https:/www.MedChemE/Sivelestat-sodium.html sodium HYPERLINK https:/www.MedChemE/Sivelestat-sodium.html (ONO5046-Na; Sodium sivelestat;

31、 EI546sodium; LY544349 sodium) Cat. No.: HY-17443ASivelestat (EI546) is a competitive inhibitor ofhuman neutrophil elastase, with an IC of 44 nM50and a K of 200 nM. Sivelestat (EI546) has theipotential for the study of acute lung injury/acuterespiratory distress syndrome or disseminatedintravascular

32、 coagulation in COVID-19.Sivelestat (EI546) sodium is a competitiveinhibitor of human neutrophil elastase, with anIC50 of 44 nM and a Ki of 200 nM.Purity: 98.26%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mgPurity: 99.13%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg HYPERLINK https:/w

33、ww.MedChemE/Sivelestat-sodium-tetrahydrate.html Sivelestat HYPERLINK https:/www.MedChemE/Sivelestat-sodium-tetrahydrate.html HYPERLINK https:/www.MedChemE/Sivelestat-sodium-tetrahydrate.html sodium HYPERLINK https:/www.MedChemE/Sivelestat-sodium-tetrahydrate.html HYPERLINK https:/www.MedChemE/Sivele

34、stat-sodium-tetrahydrate.html tetrahydrate HYPERLINK https:/www.MedChemE/Sivelestat-sodium-tetrahydrate.html (EI546 sodium tetrahydrate;LY544349 sodium tetrahydrate; ) Cat. No.: HY-17443B HYPERLINK https:/www.MedChemE/ssr69071.html SSR69071Cat. No.: HY-103445Sivelestat (EI546) sodium tetrahydrate is

35、 acompetitive inhibitor of human neutrophilelastase IC50 Ki, with an of 44 nM and a of 200 nM.SSR69071 is a potent, orally active and selectiveinhibitor of neutrophil elastase. SSR69071 reducesmyocardial infarct size followingischemia-reperfusion injury.Purity: 99.91%Clinical Data: LaunchedSize: 10 mM