Description

Product Description

Tiprelestat (CAS 820211-82-3) is a synthetic small-molecule inhibitor that specifically targets human neutrophil elastase (HNE), a serine protease implicated in multiple inflammatory pathways. Neutrophil elastase is secreted by activated neutrophils during immune responses, and while it plays a critical role in pathogen defense, its overactivation is associated with tissue damage, chronic inflammation, and autoimmune disorders.

Chemically, Tiprelestat belongs to the class of peptidomimetic inhibitors that mimic endogenous protease substrates while conferring enhanced selectivity and stability. Its molecular design allows strong inhibitory binding to the active site of neutrophil elastase, thereby blocking proteolytic cleavage of extracellular matrix components and limiting tissue degradation.

The significance of Tiprelestat in research lies in its dual pharmacological profile:

1. Anti-inflammatory activity – suppressing elastase-mediated inflammatory cascades.

2. Antimicrobial support – modulating immune pathways that interact with host defense mechanisms.

In preclinical research, Tiprelestat has shown promise across a spectrum of disease models:

• Chronic obstructive pulmonary disease (COPD) and cystic fibrosis (CF), where neutrophil elastase plays a role in airway remodeling.

• Autoimmune disorders, including rheumatoid arthritis and systemic lupus erythematosus.

• Sepsis and acute lung injury (ALI) models, in which elastase overactivation contributes to organ dysfunction.

Compared to other elastase inhibitors, Tiprelestat demonstrates:

• Greater specificity for HNE versus other proteases.

• Higher solubility and stability under experimental conditions.

• Reduced off-target cytotoxicity, ensuring reliability in long-term studies.

This unique profile makes Tiprelestat an indispensable compound in immunology, pharmacology, and translational medicine research.

Product Specifications

Tiprelestat’s high-purity production ensures reproducibility in assays and cross-laboratory experiments. Its aqueous solubility and lyophilized stability make it compatible with a wide range of biological systems. Researchers can rely on Tiprelestat as a consistent and reliable tool in both in vitro and in vivo models.

Mechanism of Action & Research Applications

Mechanism of Action:
Tiprelestat acts by irreversibly binding to the catalytic serine residue of human neutrophil elastase, preventing proteolytic degradation of structural proteins such as elastin, fibronectin, and collagen. This inhibition:

• Reduces tissue remodeling in chronic inflammation.

• Prevents alveolar wall destruction in lung disease.

• Limits immune-driven fibrosis in autoimmune pathology.

Research Applications:

1. Pulmonary Disease Research

   • COPD, cystic fibrosis, emphysema: Tiprelestat reduces airway neutrophilic inflammation and extracellular matrix breakdown.

2. Autoimmune Disorders

   • Rheumatoid arthritis: prevents joint cartilage erosion.

   • Multiple sclerosis: modulates immune-mediated damage.

3. Sepsis and Acute Lung Injury

   • Attenuates cytokine storm and neutrophil overactivation.

4. Dermatological Models

   • Psoriasis and skin inflammation, where neutrophil elastase drives keratinocyte proliferation.

5. Cancer Research

   • Investigated as a modulator of tumor microenvironment, since elastase contributes to tumor invasion and angiogenesis.

Translational Research Value:
Tiprelestat provides a platform for developing next-generation neutrophil elastase inhibitors with potential clinical utility. By bridging preclinical and translational research, it helps clarify immune-protease interactions and supports therapeutic discovery.

Side Effects (For Reference in Research Models)

While generally well tolerated in laboratory studies, Tiprelestat has demonstrated certain side effects in experimental models:

• Dose-dependent cytotoxicity at very high concentrations.

• Altered immune balance, as inhibition of elastase may reduce microbial clearance.

• Mild hepatotoxicity markers in long-term studies.

• Reduced neutrophil recruitment, potentially altering infection outcomes.

• Formulation sensitivity, with solubility and delivery methods influencing biological effects.

Researchers are advised to consider dose optimization and parallel controls when designing experiments involving Tiprelestat.

Disclaimer

For laboratory research use only. Not for human or veterinary use.

Keywords

•  CAS 820211-82-3

• Tiprelestat GMP manufacturer

• Human neutrophil elastase inhibitor

• Research use only neutrophil elastase inhibitor