Icatibant

CAS: 130308-48-4

| Product Information
Product NameIcatibant
SynonymsFirazyr, HOE-140, JE049; D-Arg-[Hyp3, Thi5, D-Tic7, Oic8]-bradykinin
CAS Number130308-48-4 (free base); acetate salt 138614-30-9
Sequence (3-Letter)H-D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Tic-Oic-Arg-OH (Hyp = 4-hydroxyproline; Thi = 3-(2-thienyl)alanine; Tic = tetrahydroisoquinoline-3-carboxylic acid; Oic = octahydroindole-2-carboxylic acid)
Sequence (1-Letter)(D-Arg)-R-P-Hyp-G-Thi-S-(D-Tic)-Oic-R
Molecular FormulaC₅₉H₈₉N₁₉O₁₃S
Molecular Weight1304.52
CategoryDrug Peptide – Bradykinin B2 Receptor Antagonist


| Specifications
Purity≥98% (by HPLC)
AppearanceWhite to off-white powder
Counter IonAcetate (salt form per specification)
Peptide Content≥80% (per specification)
SolubilitySoluble in water
Storage-20°C, desiccated, protected from light
Available Scalemg – kg (research quantities to scale-up batches)
QC DocumentationCOA, HPLC, MS identity (additional API/regulatory documentation on request)
UsageFor research and pharmaceutical development use, and as a reference standard or active pharmaceutical ingredient for manufacturing. Not for human or veterinary use; not for sale to patients. Any therapeutic use is subject to applicable regulatory approval.


FAQs

What is Icatibant?

Icatibant is a synthetic decapeptide and a selective antagonist of the bradykinin B2 receptor, known as a medicine under the brand name Firazyr and the code HOE-140 (CAS 130308-48-4; acetate salt 138614-30-9). It is derived from bradykinin and carries five non-natural amino acids, which turn it from an activator into a blocker and make it resistant to breakdown. We supply it as a white powder for research and pharmaceutical development.

How does Icatibant work?

Bradykinin is a peptide that widens blood vessels and makes them leaky, which causes swelling. Icatibant binds the bradykinin B2 receptor and blocks it, so bradykinin can no longer act there. Because it is a pure antagonist, it switches the signal off rather than on, and its non-natural amino acids let it resist the enzymes that would normally break a peptide down.

What is Icatibant used for?

Clinically, icatibant is used to treat acute attacks of hereditary angioedema in adults, a condition in which a deficiency of C1-esterase inhibitor leads to bursts of bradykinin and severe swelling. This is background information only; the material we supply is for research and pharmaceutical manufacturing use, and is not for human or veterinary use and not for sale to patients.

What grade and documentation does SynPeptide supply Icatibant in?

We supply Icatibant with a certificate of analysis, HPLC purity data, and mass-spec identity confirmation. Additional documentation for API and regulatory work is available on request, and salt form and purity can be set to your specification.

Can I order Icatibant in bulk?

Yes. We manufacture Icatibant in-house and supply from research quantities up to scale-up batches. With its several non-natural amino acids it is a demanding synthesis, and we can discuss the right approach for your scale. Contact us with your required purity and quantity for a quote.

About Icatibant

Icatibant is a synthetic decapeptide and a selective antagonist of the bradykinin B2 receptor, used to treat hereditary angioedema. It is known as a medicine under the brand name Firazyr and was originally developed as HOE-140. We supply it as a raw material for research and pharmaceutical development.

What Icatibant Is

Icatibant is a ten-residue peptide, H-D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Tic-Oic-Arg-OH, derived from the natural peptide bradykinin. It carries five non-natural amino acids, including a hydroxyproline, a thienylalanine, a tetrahydroisoquinoline-carboxylic acid, and an octahydroindole-carboxylic acid. These changes turn the molecule from an activator of the receptor into a pure blocker and make it resist enzymatic breakdown. Its free-base CAS number is 130308-48-4 (acetate salt 138614-30-9), its molecular formula is C59H89N19O13S, and its molecular weight is about 1305.

How Icatibant Works

Bradykinin is a signalling peptide that widens blood vessels and increases their leakiness, which produces swelling. Icatibant binds the bradykinin B2 receptor and blocks it competitively, with an affinity similar to bradykinin itself but without triggering the receptor. With the B2 receptor blocked, bradykinin can no longer drive the vasodilation and fluid leak that cause the swelling.

Clinical Background

Icatibant is used clinically to treat acute attacks of hereditary angioedema in adults, a disorder in which a deficiency of C1-esterase inhibitor allows bradykinin to build up and cause episodes of severe swelling. This information is provided as scientific and reference background only. The material supplied by SynPeptide is intended for research and pharmaceutical manufacturing, is not for human or veterinary use, and is not for sale to patients; any therapeutic use is subject to applicable regulatory approval.

Grade, Quality, and Documentation

Because icatibant contains several non-natural amino acids, it calls for careful synthesis and purification. We supply it with a certificate of analysis, HPLC purity data, and mass-spectrometry identity confirmation, with further documentation available to support active pharmaceutical ingredient and regulatory work, and purity and salt form set to your specification.

Sourcing and Custom Synthesis

We manufacture Icatibant by solid-phase synthesis, including its non-natural and D-amino acid residues, and supply it from research quantities through to scale-up batches. For related capabilities, see drug peptides, custom peptide synthesis, peptide modification, and our peptide CDMO services. Material is supplied for research and pharmaceutical manufacturing use only.

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