Ecallantide

HAE is caused by a mutation of the C1-inhibitor gene. Defective or missing C1-inhibitor permits activation of kallikrein, a protease that is responsible for liberating bradykinin from its precursor kininogen. An excess of bradykinin leads to fluid leakage from blood vessels, causing swelling of tissues typical of HAE.Ecallantide suppresses this pathogenetic mechanism by selectively and reversibly inhibiting the activity of plasma kallikrein.

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CAT#10-101-160
CAS460738-38-9
Background

Ecallantide, as known as Kalbitor, is a drug used for the treatment of hereditary angioedema (HAE) and in the prevention of blood loss in cardiothoracic surgery. It is an inhibitor of the protein kallikrein and a 60-amino acid polypeptide which was developed from a Kunitz domain through phage display to mimic antibodies inhibiting kallikrein. HAE is caused by a mutation of the C1-inhibitor gene. Defective or missing C1-inhibitor permits activation of kallikrein, a protease that is responsible for liberating bradykinin from its precursor kininogen. An excess of bradykinin leads to fluid leakage from blood vessels, causing swelling of tissues typical of HAE. Ecallantide suppresses this pathogenetic mechanism by selectively and reversibly inhibiting the activity of plasma kallikrein.  >> Read More

Synonyms/AliasDX-88 cpd;EPI-KAL-2;Kalbitor
M.F/FormulaC305H442N88O91S8
M.W/Mr.7053.83
SequenceEAMHSFCAFKADDGPCRAAHPRWFFNIFTRQCEEFIYGGCEGNQNRFESLEECKKMCTRD(Disulfide bridge: 7-57; 16-40; 32-53)
Labeling TargetPlasma kallikrein
ApplicationTreatment of hereditary angioedema, Reduction of blood loss during cardiothoracic surgery [plasma kallikrein inhibitor]
ActivityInhibitor
Biological ActivityEcallantide is a highly specific recombinant plasma kallikrein inhibitor developed for treatment of hereditary angioedema (HAE).
Areas of InterestHereditary angioedema
FunctionsSerine-type endopeptidase activity
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