Tenivastatin calcium is a HMG-CoA reductase inhibitor. Tenivastatin calcium can reduce blood lipid level can be used for the research of hyperlipidemia.

PROTAC HIF-1α degrader-2 is a highly efficient and selective PROTAC degrader targeting HIF-1α. PROTAC HIF-1α degrader-2 promotes HIF-1α degradation via the ubiquitin-proteasome pathway by facilitating the formation of a HIF-1α/VHL ternary complex. PROTAC HIF-1α degrader-2 inhibits HeLa cell proliferation, migration, and colony formation, and induces apoptosis. PROTAC HIF-1α degrader-2 reduces p-MEK and p-AKT expression in the MAPK and PI3K/AKT pathways. PROTAC HIF-1α degrader-2 can be used for the study of cervical cancer. (Pink: HIF-1α ligand ; Blue: VHL ligand ; Black: linker).

Neutrophil elastase-IN-7 (Compound 12) is an effective inhibitor of neutrophil elastase (HNE), with an IC50 value of 0.54 μM. Neutrophil elastase-IN-7 also exhibits significant inhibitory activity against various coagulation proteins, with the IC50 values for thrombin, FXa, FXIa, and FXIIIa being 8.2, 12.7, 1.2, and 5.7 μM, respectively. Neutrophil elastase-IN-7 can be used for research on inflammation, innate immune responses, and tissue remodeling.

ICI-200880 is a potent, selective and reversible human neutrophil elastase (HNE) inhibitor. ICI-200880 is promising for research of inflammatory lung diseases related to neutrophil elastase, such as chronic obstructive pulmonary disease (COPD) and cystic fibrosis (CF).

KRP-109 is a neutrophil elastase (NE) inhibitor with activity in reducing lung inflammation. KRP-109 improves survival in mouse models and reduces the number of neutrophils and inflammation in the alveolar walls. KRP-109 significantly reduced cell and neutrophil counts in bronchoalveolar lavage fluid, as well as cytokine levels such as interleukin 1β and macrophage inflammatory protein 2. KRP-109 can be used in the research of severe pneumonia.

(S)-MDL-101146 is the S-isomer of MDL-101146. MDL-101146 is an orally active, competitive and reversible inhibitor against human neutrophil elastase (HNE) with a Ki value of 25 nM. MDL-101146 inhibits HNE-induced hemorrhage in hamsters. MDL-101146 is promising for research of emphysema, rheumatoid arthritis, chronic bronchitis, cystic fibrosis, adult respiratory distress syndrome and glomerulonephritis.

(R)-MDL-101146 is the R-isomer of MDL-101146. MDL-101146 is an orally active, competitive and reversible inhibitor against human neutrophil elastase (HNE) with a Ki value of 25 nM. MDL-101146 inhibits HNE-induced hemorrhage in hamsters. MDL-101146 is promising for research of emphysema, rheumatoid arthritis, chronic bronchitis, cystic fibrosis, adult respiratory distress syndrome and glomerulonephritis.

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.

MeO-Suc-Ala-Ala-Pro-Ala-CMK (MSACK) is an inhibitor of human neutrophil elastase (HNE), with an IC50 of 20.3 μM. MeO-Suc-Ala-Ala-Pro-Ala-CMK can inhibit the hydrolysis of substrates such as elastin in lung tissue by HNE. MeO-Suc-Ala-Ala-Pro-Ala-CMK can be used in the research of related diseases such as chronic obstructive pulmonary disease (COPD).

TEI-8362 is a potent, selective inhibitor of human neutrophil elastase (HNE) with Ki value of 1.38 nM and IC50 of 1.9 nM.

Lonodelestat (POL6014) is a potent, orally active and selective peptide inhibitor of human neutrophil elastase (hNE).

BAY-678 is a cell-permeable inhibitor of human neutrophil elastase (HNE).

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.

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.

Alvelestat (tosylate) is an orally bioavailable, affinity and selective inhibitor of neutrophil elastase (NE) with a pIC50 value of 7.9 nM, a Ki value of 9.4 nM and a Kd value of 9.5 nM.

Bay-8040 is a potent, selective human neutrophil elastase (HNE) inhibitor with IC50 of 28 nM; displays no significant inhibition toward 68 other pharmacologically relevant targets (>10 uM), and a panel of related serine proteases; shows in vivo efficacy with regard to decreasing cardiac remodeling and amelioration of cardiac function in monocrotaline-induced rat model for pulmonary arterial hypertension.

Cyclotheonellazole A is a natural macrocyclic peptide and a potent elastase inhibitor (IC50=0.034 nM). Cyclotheonellazole A inhibits chymotrypsin with an IC50 value of 0.62 nM.

SSR69071 is a potent, orally active and selective inhibitor of neutrophil elastase. SSR69071 reduces myocardial infarct size following ischemia-reperfusion injury. 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.

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

AE-3763 is a peptide-based human neutrophil elastase inhibitor with an IC50 of 29 nM.

Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate 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 quarterhydrate has a potent anti-inflammatory activity.

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.

DMP 777(L-694458) is a potent, selective, and orally active human leukocyte elastase (HLE) inhibitor.

BAY 85-8501 (BAY85-8501) is a potent, selective human neutrophil elastase (HNE) inhibitor with IC50 of 65 pM.

A potent, selective and orally active human neutrophil elastase (HNE) inhibitor with Ki of 12 nM.