Elastases are proteinases capable of solubilizing fibrous elastin. Elastases may belong to the class of serine proteinases, cysteine proteinases and metalloproteinases. Mammalian elastases occur mainly in the pancreas and the phagocytes. Among non-mammalian elastases there is a great variety of bacterial metallo and serine elastases. The elastolytic activity varies from one elastase to another and is usually not correlated with the catalytic efficiency of these proteinases. One may measure this activity using native or labelled elastins. With pure elastases one may use synthetic substrates. There is a large number of natural (proteins) and synthetic elastase inhibitors. Elastases play a pathologic role in pulmonary emphysema, cystic fibrosis, infections, inflammation and atherosclerosis.


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Panicolin

Skullcapflavone I can be isolated from A. nallamalayana. Skullcapflavone I inhibits collagenase and elastase enzyme with IC50s of 106.74 μM and 186.70 μM. Skullcapflavone I has anticancer activities by down-regulating miR-23a[1].

  • CAS Number: 41060-16-6
  • MF: C17H14O6
  • MW: 314.29
  • Catalog: MicroRNA
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 573.6±50.0 °C at 760 mmHg
  • Melting Point: 254-256℃
  • Flash Point: 215.5±23.6 °C

Alvelestat

Alvelestat (AZD9668) is a novel, oral inhibitor of neutrophil elastase (NE) with the pIC50 of 7.9 for Human NE.IC50 Value: 7.9 ± 0.12 (pIC50, Human NE); 4.9 nM (Ki value, Human NE) [1]Target: Neutrophil elastasein vitro: AZD9668 had a high binding affinity for human NE (KD = 9.5 nM) and potently inhibited NE activity. The calculated pIC50 (IC50) and Ki values for AZD9668 for human NE were 7.9 (12 nM) and 4.9 nM, respectively. In contrast to earlier NE inhibitors, the interaction between AZD9668 and NE was rapidly reversible. AZD9668 was also highly selective for NE over other neutrophil-derived serine proteases. In cell-based assays, AZD9668 inhibited plasma NE activity in zymosan-stimulated whole blood. In isolated human polymorphonuclear cells, AZD9668 inhibited NE activity on the surface of stimulated cells and in the supernatant of primed, stimulated cells.AZD9668 showed good crossover potency to NE from other species [1]. in vivo: Six hundred and fifteen patients were randomised: placebo (302), AZD9668 60 mg bid (313). AZD9668 showed no effect on lung function: change in mean pre-bronchodilator FEV1 versus placebo was 0.01L (95% confidence interval: -0.03, 0.05; p=0.533). AZD9668 did not significantly improve respiratory signs and symptoms, SGRQ-C score or time to first exacerbation. Adverse events were similar for AZD9668 and placebo [2]. AZD9668 was well tolerated at single doses up to 150 mg and multiple doses up to 70 mg twice daily. PK were dose linear; median time to peak plasma concentration was reached at 0.5 - 1.5 hours and the short elimination half-life was consistent with twice daily dosing. Steady state was reached by Day 2 of twice daily dosing with negligible accumulation. Approximately 40% of AZD9668 was eliminated renally as unchanged compound. Ex vivo zymosan-stimulated inhibition of NE activity was dose-dependent, with maximal inhibition achieved at 60 mg [4].Toxicity: A total of 838 patients were randomised to AZD9668 5 mg bid (212 patients), 20 mg bid (206 patients), 60 mg bid (202 patients) or placebo (218 patients). AZD9668 showed no effect on lung function, respiratory signs and symptoms, QoL or biomarkers [3].Clinical trial: Phase II study of a neutrophil elastase inhibitor (AZD9668) in patients with bronchiectasis.

  • CAS Number: 848141-11-7
  • MF: C25H22F3N5O4S
  • MW: 545.534
  • Catalog: Elastase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 780.4±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 425.8±32.9 °C

Chrysophanol 8-O-glucoside

Chrysophanol 8-O-glucoside, from the roots of Rumex acetosa, shows moderate elastase inhibition activity[1].

  • CAS Number: 13241-28-6
  • MF: C21H20O9
  • MW: 416.378
  • Catalog: Elastase
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 763.2±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 272.8±26.4 °C

Lodelaben

Lodelaben is a human neutrophil elastase inhibitor with an IC50 and Ki of 0.5 and 1.5 μM, respectively.

  • CAS Number: 111149-90-7
  • MF: C25H41ClO3
  • MW: 425.04400
  • Catalog: Elastase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ZD-0892

ZD-0892 is a selective and potent inhibitor of a neutrophil elastase with Kis of 6.7 and 200 nM for human neutrophil elastase and porcine pancreatic elastase, respectively.

  • CAS Number: 171964-73-1
  • MF: C24H32F3N3O5
  • MW: 499.52
  • Catalog: Elastase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

JCP174

JCP174 is an inhibitor of palmitoyl protein thioesterase-1 (TgPPT1), a depalmitoylase in the parasite T. gondii[1]. JCP174 is also an inhibitor of porcine pancreatic elastase and human leukocyte elastase[2][3].

  • CAS Number: 126062-19-9
  • MF: C12H12ClNO3
  • MW: 253.682
  • Catalog: Elastase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 463.4±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 234.1±28.7 °C

FK706

FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect[1][2].

  • CAS Number: 144055-55-0
  • MF: C26H32F3N4NaO7
  • MW: 592.54
  • Catalog: Elastase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Suc-Ala-Ala-Pro-Abu-pNA trifluoroacetate salt

Suc-AAP-Abu-pNA (Colorimetric Elastase Substrate) is a specific substrate for pancreatic elastase (Km = 100 μM; Kcat/Km = 35,300 s-1 M-1 for rat pancreatic elastase; Km = 30 μM; Kcat/Km = 351,000 s-1 M-1 for porcine pancreatic elastase). Suc-AAP-Abu-pNA also promotes OPC migration[1].

  • CAS Number: 108392-27-4
  • MF: C25H34N6O9
  • MW: 562.572
  • Catalog: Elastase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 1014.2±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 567.1±34.3 °C

Tutuilamide A

Tutuilamide A is a potent porcine pancreatic elastase (PPE) inhibitor, with an IC50 of 1.2 nM. Tutuilamide A also inhibits human neutrophil elastase (HNE; IC50=0.73 nM) and kallikrein 7 (KLK7; IC50=5.0 nM)[1].

  • CAS Number: 2756129-42-5
  • MF: C51H69ClN8O12
  • MW: 1021.59
  • Catalog: Elastase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Secologanoside

Secologanoside is a triterpenoid isolated from Poraqueiba sericea, weakly inhibits elastase with an IC50 of 164 μg/mL. Secologanoside is moderate cytotoxic to fibroblasts[1].

  • CAS Number: 59472-23-0
  • MF: C16H22O11
  • MW: 390.34
  • Catalog: Elastase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GW311616

GW311616 is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM; free base form of GW311616A.IC50 value: 22 nM [1]Target: neutrophil elastaseThe HNE inhibitor GW311616A is selective over other human serine proteases (IC50 values >100 uM for trypsin, cathepsin G, and plasmin, >3 mM for chymotrypsin and tissue plasminogen activator). Acetylcholinesterase is not inhibited by GW311616A at 100 uM.GW311616A is more potent than thetrifluoromethylketone inhibitor ZD8321 (Ki=13 nM). GW311616A is orallybioavailable in rat, dog (Table 4) and hamster despite moderate to high plasmaclearance, which indicates that clearance is predominantly extrahepatic.

  • CAS Number: 198062-54-3
  • MF: C19H31N3O4S
  • MW: 397.53
  • Catalog: Elastase
  • Density: N/A
  • Boiling Point: 604.3ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 319.3ºC

SPCK

MeOSuc-AAPV-CMK (Elastase Inhibitor III) is an elastase inhibitor. MeOSuc-AAPV-CMK also inhibits cathepsin G and proteinase 3.MeOSuc-AAPV-CMK blocks the cleavage of adiponectin by leukocyte elastase[1].

  • CAS Number: 65144-34-5
  • MF: C22H35ClN4O7
  • MW: 502.98900
  • Catalog: Cathepsin
  • Density: 1.234g/cm3
  • Boiling Point: 809.4ºC at 760 mmHg
  • Melting Point: 159-161ºC
  • Flash Point: 443.3ºC

Elasnin

Elasnin is a selective granulocyte elastase inhibitor. Elasnin is almost ineffective for pancreatic elastase, trypsin, chymotrypsin, thermolysin and papain[1].

  • CAS Number: 68112-21-0
  • MF: C24H40O4
  • MW: 392.57
  • Catalog: Elastase
  • Density: 1.001g/cm3
  • Boiling Point: 521ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 166.6ºC

Sivelestat Sodium

Sivelestat sodium(ONO5046; LY544349; EI546) is a competitive inhibitor of human neutrophil elastase(IC50 = 44 nM; Ki=200 nM); also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse.IC50 value: 44 nM [1]Target: neutrophil elastaseONO-5046 did not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 microM. In in vivo studies, ONO-5046 suppressed lung hemorrhage in hamster (ID50 = 82 micrograms/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6 mg/kg) by intravenous administration, both of which were induced by human neutrophil elastase [1]. Sivelestat sodium hydrate is an anti-neutrophil elastase inhibitor and may be one of the treatment options for acute respiratory failure due to pneumocystis pneumonia in AIDS patients [2].

  • CAS Number: 150374-95-1
  • MF: C20H21N2NaO7S
  • MW: 456.445
  • Catalog: Elastase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ONO 6818

Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity[1][2][3][4].

  • CAS Number: 208848-19-5
  • MF: C23H28N6O4
  • MW: 452.50600
  • Catalog: Elastase
  • Density: 1.32g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DMP 777

DMP 777 is a potent, selective, and orally active human leukocyte elastase (HLE) inhibitor.

  • CAS Number: 157341-41-8
  • MF: C31H40N4O6
  • MW: 564.67200
  • Catalog: Elastase
  • Density: 1.227g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ZD8321

ZD8321 is a potent inhibitor of human Neutrophil elastase (NE) with a Ki of 13±1.7 nM.

  • CAS Number: 182073-77-4
  • MF: C18H28F3N3O5
  • MW: 423.427
  • Catalog: Elastase
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 573.9±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 300.9±30.1 °C

BAY-85-8501

BAY-85-8501 is a selective and potent inhibitor of Human Neutrophil Elastase (HNE), with an IC50 of 65 pM.

  • CAS Number: 1161921-82-9
  • MF: C22H17F3N4O3S
  • MW: 474.456
  • Catalog: Elastase
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 626.7±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 332.8±31.5 °C

GW311616A

GW311616A(GW311616 Hcl) is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM.IC50 value: 22 nM [1]Target: neutrophil elastaseThe HNE inhibitor GW311616A is selective over other human serine proteases (IC50 values >100 uM for trypsin, cathepsin G, and plasmin, >3 mM for chymotrypsin and tissue plasminogen activator). Acetylcholinesterase is not inhibited by GW311616A at 100 uM.GW311616A is more potent than thetrifluoromethylketone inhibitor ZD8321 (Ki=13 nM). GW311616A is orallybioavailable in rat, dog (Table 4) and hamster despite moderate to high plasmaclearance, which indicates that clearance is predominantly extrahepatic.

  • CAS Number: 197890-44-1
  • MF: C19H32ClN3O4S
  • MW: 433.993
  • Catalog: Elastase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Sivelestat sodium salt hydrate

Sivelestat(ONO5046; LY544349; EI546) is a competitive inhibitor of human neutrophil elastase(IC50 = 44 nM; Ki=200 nM); also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse.IC50 value: 44 nM [1]Target: neutrophil elastaseONO-5046 did not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 microM. In in vivo studies, ONO-5046 suppressed lung hemorrhage in hamster (ID50 = 82 micrograms/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6 mg/kg) by intravenous administration, both of which were induced by human neutrophil elastase [1]. Sivelestat sodium hydrate is an anti-neutrophil elastase inhibitor and may be one of the treatment options for acute respiratory failure due to pneumocystis pneumonia in AIDS patients [2].

  • CAS Number: 127373-66-4
  • MF: C20H22N2O7S
  • MW: 434.463
  • Catalog: Elastase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SSR 69071

SSR69071 is a potent, orally active and selective inhibitor of neutrophil elastase. SSR69071 reduces myocardial infarct size following ischemia-reperfusion injury[1]. SSR69071 displays a higher affinity for human elastase (Ki=0.0168 nM) than for rat (Ki=3 nM), mouse (Ki=1.8 nM), and rabbit (Ki= 58 nM) elastases[2].

  • CAS Number: 344930-95-6
  • MF: C27H32N4O7S
  • MW: 556.63100
  • Catalog: Elastase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SP-Chymostatin B

SP-Chymostatin B is a potent inhibitor of many proteases, including chymotrypsin, papain, chymotrypsin-like serine proteinases, chymases, and lysosomal cysteine proteinases. It weakly inhibits human leucocyte elastase. It is effective at a final concentration of 100 to 200 μg/ml (10 to 100 μM).

  • CAS Number: 70857-49-7
  • MF: C30H41N7O6
  • MW: 595.701
  • Catalog: Elastase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KLK7/ELA2-IN-1

KLK7/ELA2-IN-1 is a potent kallikrein-related peptidase 7 (KLK7) and epidermal elastase 2 (ELA2) inhibitor with IC50s of 6 nM and 55 nM, respectively (WO2009024527A1, Example 4)[1].

  • CAS Number: 1122484-55-2
  • MF: C46H72N8O12
  • MW: 929.11
  • Catalog: Elastase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Elastatinal

Elastatinal is a potent and competitive inhibitor of elastase, with a Ki of 0.21 μM. Elastatinal more potently inhibits pancreatic elastase versus leucocyte elastase. Elastatinal shows no activity on human leucocyte chymotrypsin-like protease[1][2][3][4].

  • CAS Number: 51798-45-9
  • MF: C21H36N8O7
  • MW: 512.56
  • Catalog: Elastase
  • Density: 1.44 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Suc-Ala-Pro-Ala-AMC

Suc-Ala-Pro-Ala-AMC is a tripeptide substrate of elastase[1].

  • CAS Number: 88467-44-1
  • MF: C25H30N4O8
  • MW: 514.52800
  • Catalog: Elastase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tiprelestat

Tiprelestat is a potent human neutrophil elastase inhibitor. Tiprelestat has antimicrobial and anti-inflammatory activities. Tiprelestat can be used in the research of inflammation/immune disease[1].

  • CAS Number: 820211-82-3
  • MF: C254H416N72O75S10
  • MW: 5999.09
  • Catalog: Elastase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BAY 678

BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).

  • CAS Number: 675103-36-3
  • MF: C20H15F3N4O2
  • MW: 400.35
  • Catalog: Elastase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

19 alpha-Hydroxyasiatic acid

19α-Hydroxyasiatic acid, a natural triterpenoid, possesses anti-elastase activity[1].

  • CAS Number: 70868-78-9
  • MF: C30H48O6
  • MW: 504.70
  • Catalog: Elastase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 283℃
  • Flash Point: N/A

MDL 101146

MDL 101146 is an orally active neutrophil elastase inhibitor. MDL 101146 inhibits neutrophil elastase for human with a Ki value of 25 nM. MDL 101146 can be used for the research of arthritis[1][2].

  • CAS Number: 149859-17-6
  • MF: C29H37F5N4O6
  • MW: 632.61900
  • Catalog: Elastase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BAY-678 racemate

BAY-678 racemate is a racemate of BAY-678. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).

  • CAS Number: 675103-35-2
  • MF: C20H15F3N4O2
  • MW: 400.35
  • Catalog: Elastase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A