Icatibant (Firazyr) is a synthetic peptidomimetic drug consisting of ten amino acids, and acts as an effective and specific antagonist of bradykinin B2 receptors. It has been approved in the EU for use in hereditary angioedema, and is under investigation for a number of other conditions in which bradykinin is thought to play a significant role.
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M.F/Formula | C59H89N19O13S |
M.W/Mr. | 1304.52 |
Sequence | D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-Tic-Oic-Arg |
Labeling Target | B2 bradykinin receptor |
Application | Approved for use in acute attacks of hereditary angioedema (HAE). Investigated for use/treatment in angioedema, liver disease, and burns and burn infections. |
Appearance | Solid powder |
Purity | >98% (or refer to the Certificate of Analysis) |
Activity | Antagonist |
Biological Activity | Icatibant (HOE-140) is a potent and specific peptide antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively. |
Areas of Interest | Hereditary angioedema |
Functions | Type 1 angiotensin receptor binding |
Target | Bradykinin Receptor |
Source# | Synthetic |
Long-term Storage Conditions | Soluble in DMSO. |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
Short-term Storage Conditions | Dry, dark and at 0 - 4 °C |
Solubility | -20 °C |
Organism | Human |
BoilingPoint | N/A |
ShelfLife | >2 years if stored properly |
References | Icatibant (also called JE049 or HOE140) is a synthetic decapeptide that has a similar structure as bradykinin but contains 5 nonproteinogenic amino acids (D-Arg, L-Hyp, L-Thi, D-Tic, and L-Oic). It is stable and not degraded by bradykinin-cleaving enzymes like carboxypeptidase N (or kininase I) and angiotensin converting enzyme (or kininase II). The study drug was provided by the Jerini AG (Berlin, Germany). Treatment of acute edema attacks in hereditary angioedema with a bradykinin receptor-2 antagonist (Icatibant) Icatibant is a selective bradykinin B2 receptor antagonist with, like bradykinin itself, an affinity for the B2 receptor. It does not interact with bradykinin B1 receptors or other peptide receptors. Icatibant reverses increased vascular permeability in C1 esterase inhibitor–knockout mice, inhibits bradykinin-induced vasodilation in humans and, in a phase 1 study, showed dose- and time-dependent inhibition of bradykinin-induced effects in vivo. In a phase 2 study, symptoms improved significantly after open-label treatment with icatibant in 15 patients with hereditary angioedema having acute cutaneous or abdominal attacks. Icatibant, a New Bradykinin-Receptor Antagonist, in Hereditary Angioedema |
Melting Point | N/A |
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