Ecallantide (CAS No. 460738-38-9) | High-Purity Plasma Kallikrein Inhibitor

描述

Product Description

Ecallantide is a recombinant peptide inhibitor of human plasma kallikrein, developed to target the bradykinin pathway, which is centrally involved in the pathophysiology of hereditary angioedema (HAE) and other disorders associated with vascular permeability and inflammation. Known under the research name DX-88, Ecallantide represents a class of selective kallikrein inhibitors designed to disrupt abnormal bradykinin production while preserving the physiological functions of other proteases.

The importance of Ecallantide lies in its specificity. Unlike broad-spectrum protease inhibitors, Ecallantide exhibits nanomolar affinity for plasma kallikrein, providing a targeted approach for dissecting the role of this enzyme in complement activation, contact system biology, and vascular physiology.

Scientific Significance

The kallikrein-kinin system regulates a range of physiological responses including:

• Vasodilation

• Inflammation and edema formation

• Pain perception

• Blood coagulation and fibrinolysis balance

Excessive bradykinin production has been directly implicated in diseases such as hereditary angioedema, septic shock, ischemia-reperfusion injury, and certain inflammatory disorders. By blocking kallikrein-mediated cleavage of high-molecular-weight kininogen (HMWK), Ecallantide prevents excessive bradykinin release, providing a controlled model for studying vascular leakage, inflammatory cascades, and immune modulation.

Broader Research Relevance

While Ecallantide has been most closely linked with angioedema research, its potential extends to multiple areas:

• Thrombosis and coagulation studies

• Complement system regulation

• Acute inflammatory disease models

• Autoimmune pathologies

• Sepsis and shock research

• Target validation for drug development

This makes Ecallantide a valuable tool compound in both preclinical and translational immunology.

Product Specifications

Notes on Specifications

• Molecular Features: Ecallantide is a recombinant protein with a defined amino acid sequence designed for high affinity binding to plasma kallikrein.

• Purity Control: HPLC and LC-MS are used to confirm ≥98% batch quality.

• Formulation: Provided as a lyophilized powder, ensuring long-term stability and ease of transport.

• Compatibility: Can be reconstituted in physiological buffers for in vitro and in vivo studies.

Mechanism of Action & Research Applications

Mechanism of Action

Ecallantide works by binding to plasma kallikrein with high affinity, preventing it from cleaving high-molecular-weight kininogen (HMWK) into bradykinin. This inhibition blocks the overproduction of bradykinin, thereby preventing downstream events such as:

• Increased vascular permeability

• Edema formation

• Uncontrolled inflammation

Unlike bradykinin receptor antagonists (which block the receptor), Ecallantide intervenes upstream, targeting the enzyme responsible for bradykinin generation. This makes it a powerful pathway-specific inhibitor for dissecting kallikrein-driven disease processes.

Research Applications

1. Hereditary Angioedema (HAE) Models – Used to study prevention of acute swelling episodes.

2. Bradykinin Biology – Helps investigate vascular leakage, hypotension, and pain signaling.

3. Inflammatory Disease Research – Relevant in models of arthritis, colitis, and sepsis.

4. Complement System Modulation – Allows exploration of the crosstalk between kallikrein and complement activation.

5. Drug Development – Serves as a reference compound for benchmarking new kallikrein inhibitors.

6. Thrombosis & Coagulation – Studied for its potential role in balancing hemostasis and fibrinolysis.

7. Cardiovascular Research – Offers insights into endothelial function and vascular reactivity.

Translational Insights

Because plasma kallikrein is implicated in both rare genetic disorders (HAE) and systemic inflammatory conditions, Ecallantide serves as a critical research tool for bridging molecular biology with clinical immunology.

Side Effects (For Research Context Only)

Although Ecallantide is a research compound and not intended for clinical use, reported data from preclinical and investigational contexts provide insights into potential side effects:

1. Hypersensitivity Reactions – As a recombinant protein, it may trigger allergic responses in animal models.

2. Injection Site Reactions – Local swelling, erythema, or discomfort in experimental settings.

3. Immune Responses – Risk of anti-drug antibody (ADA) generation in prolonged models.

4. Vascular Effects – Hypotension or altered vascular tone due to interference with kallikrein-bradykinin signaling.

5. Complement Cascade Interference – Possible unintended effects on coagulation and fibrinolysis.

6. Species Variability – Differential response based on kallikrein isoforms across species.

These effects should be interpreted strictly in the context of laboratory research, not therapeutic application.

Disclaimer

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

Keywords

• Ecallantide

• Ecallantide CAS 460738-38-9

• DX-88 peptide inhibitor

• Plasma kallikrein inhibitor

• Bradykinin pathway peptide

• Kallikrein inhibitor for research

• GMP-grade recombinant peptide

• Inflammation research peptide

• Angioedema peptide inhibitor

• Peptide-based kallikrein blockade