| Identification | Back Directory | [Name]
ecallantide | [CAS]
460738-38-9 | [Synonyms]
DX 88
Cys16-Cys40
ecallantide
Cys32-Cys53)
ecallantide USP/EP/BP
H-Glu-Ala-Met-His-Ser-Phe-Cys-Ala-Phe-Lys-Ala-Asp-Asp-Gly-Pro-Cys-Arg-Ala-Ala-His-Pro-Arg-Trp-Phe-Phe-Asn-Ile-Phe-Thr-Arg-Gln-Cys-Glu-Glu-Phe-Ile-Tyr-Gly-Gly-Cys-Glu-Gly-Asn-Gln-Asn-Arg-Phe-Glu-Ser-Leu-Glu-Glu-Cys-Lys-Lys-Met-Cys-Thr-Arg-Asp-OH(Disulfide bridge：Cys7-Cys57 | [Molecular Formula]
C305H442N88O91S8 | [MOL File]
460738-38-9.mol | [Molecular Weight]
7053.83 |
| Chemical Properties | Back Directory | [Sequence]
Glu-Ala-Met-His-Ser-Phe-Cys-Ala-Phe-Lys-Ala-Asp-Asp-Gly-Pro-Cys-Arg-Ala-Ala-His-Pro-Arg-Trp-Phe-Phe-Asn-Ile-Phe-Thr-Arg-Gln-Cys-Glu-Glu-Phe-Ile-Tyr-Gly-Gly-Cys-Glu-Gly-Asn-Gln-Asn-Arg-Phe-Glu-Ser-Leu-Glu-Glu-Cys-Lys-Lys-Met-Cys-Thr-Arg-Asp (Disulfide bond:Cys1-Cys6, Cys2-Cys4, Cys3-Cys5) |
| Hazard Information | Back Directory | [Description]
Ecallantide, also known as DX-88, was approved in 2009 in the
United States for treatment of hereditary angioedema (HAE), a condition
characterized by episodic attacks of localized edema in cutaneous
and mucosal tissues. HAE results from deficiencies or disorders of C1-esterase inhibitor protein (C1-
1NH). Mutation of the gene that encodes C1-1NH causes the lack or
altered activity of the serine protease, C1-1NH. C1-1NH regulates the
kallikrein–kinin (contact activation) and complement cascade systems.
Ecallantide (DX-88) was designed to inhibit the action of
plasma kallikrein. Ecallantide is a potent and selective inhibitor of
plasma kallikrein with a Ki= 25 pM. The discovery program that
identified ecallantide used phage display technology and a library of
designed variants of the first Kunitz domain of TFPI. Ecallantide, a
60-amino acid peptide, with 3-disulfide bonds, differs from TFPI by
7-amino acids. Ecallantide has been developed as a subcutaneous
administered formulation. | [Originator]
Dyax Corp. (United States) | [Uses]
Treatment of hereditary angioedema; reduction of blood loss during cardiothoracic surgery (plasma kallikrein inhibitor). | [Brand name]
Kalbitor | [Synthesis]
Dissolve 150 g of the linear crude peptide of eicosapentin in 150 L of buffer system, which was an aqueous solution of 0.1 mM ammonium acetate, 3 times the amount of DTT of the linear crude peptide (in substance), pH 7.8, and place it in the open mouth at |
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