Lodelaben

SKU: orb1709253

Description

Lodelaben (Declaben, SC-39026) is a specific and potent reversible, non-competitive inhibitor of human neutrophil elastase (HNE), with an IC50 of 0.5 µM and a Ki of 1.5 µM. This small molecule is a valuable research tool for studying HNE's role in inflammatory diseases such as COPD and cystic fibrosis in both in vitro and in vivo experimental models.

Research Area

Protein Biochemistry

Key Properties

• CAS Number: 111149-90-7
• MW: 425.04
• Purity: 99.62% (May vary between batches)
• Formula: C₂₅H₄₁ClO₃
• SMILES: O=C(O)C1=CC=C(C=C1Cl)C(O)CCCCCCCCCCCCCCCCC
• Target: Serine Protease

Bioactivity

• Target IC50:
  Elastase:0.5 μM|Elastase:1.5 μM (Ki)
• In Vivo:
  Methods: Lodelaben (SC-39026) (40 mg/kg, gavage, 8 days) was administered to male Sprague-Dawley rats 8 days after a single subcutaneous injection of monocrotaline (60 mg/kg) or saline. Thirteen days after injection, an indwelling cardiovascular catheter was inserted under pentobarbital anesthesia, and 15 days after injection, pulmonary and systemic hemodynamic measurements were recorded while the animals were awake, and at necropsy, the lungs were perfused and evaluated by light and electron microscopy using morphometric techniques. Results: Saline-injected rats given Lodelaben or vehicle were similar in all characteristics evaluated. In contrast, mean pulmonary artery pressure was significantly lower in monocrotaline rats injected with SC-39026 than in rats given vehicle (21.0 +/- 1.6 vs. 27.5 +/- 0.8 mm Hg, p less than 0.05), which was associated with a significant reduction in the number of muscularized arteries at the alveolar wall level (r2 = 0.89, p less than 0.001).
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• In Vitro:
  Lodelaben is a human neutrophil elastase inhibitor with IC50 and Ki50 of 0.5 and 1.5 μM, respectively. Lodelaben can inhibit human neutrophil elastase (HNE) in a non-competitive manner.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

elastase, Lodelaben, Declaben, SC39026, SC-39026, SC 39026

Compound Identifiers

PubChem CID

56557