Icatibant

Icatibant is a potent bradykinin B2 receptor antagonist peptide for inflammation and allergy research. Buy Icatibant peptide from a reliable peptide supplier to support biomedical studies.

Designed for biological research and industrial applications, not intended for individual clinical or medical purposes.

CAT No: 10-101-163

CAS No:130308-48-4

Synonyms/Alias:Icatibant;130308-48-4;Firazyr;icatibanto;HOE 140;UNII-7PG89G35Q7;7PG89G35Q7;Hoechst 140;DTXSID20903963;HOE140;Icatibant [INN];(R)-ARGINYL-(S)-ARGINYL-(S)-PROLYL-(2S,4R)-(4-HYDROXYPROLYL)GLYCYL-(S)-(3-(2-THIENYL)ALANYL)-(S)-SERYL-(R)-((1,2,3,4-TETRAHYDRO-3-ISOQUINOLYL)CARBONYL)-(2S,3AS,7AS)-((HEXAHYDRO-2-INDOLINYL)CARBONYL)-(S)-ARGININE;Icatibant [INN:BAN];icatibantum;icatibant-acetate;D-Arg-(Hyp3,Thi5,D-Tic7,Oic8)BK;JE 049;Icatibant (Standard);Icatibant HOE 140;ICATIBANT [MI];ICATIBANT [VANDF];HOE-140 (Icatibant);ICATIBANT [WHO-DD];ICATIBANT [EMA EPAR];HOE 140 TFA;CHEMBL2028850;SCHEMBL21495177;B06AC02;DTXCID901331902;BDBM50403371;BDBM50406750;HY-17446R;AKOS040741862;AT24149;CS-3381;DB06196;NCGC00390805-02;DA-64221;HY-17446;HOE 140, >=94%;EN300-18166877;Q902379;BRD-K63772874-001-01-4;BRD-K63772874-001-02-2;L-ARGININE, D-ARGINYL-L-ARGINYL-L-PROLYL-TRANS-4-HYDROXY-L-PROLYLGLYCYL-3-(2-THIENYL)-L-ALANYL-L-SERYL-D-1,2,3,4-TETRAHYDRO-3-ISOQUINOLINECARBONYL-L-(2.ALPHA.,3A.BETA.,7A.BETA.)-OCTAHYDRO-1H-INDOLE-2-CARBONYL-;L-Arginine, D-arginyl-L-arginyl-L-prolyl-trans-4-hydroxy-L-prolylglycyl-3-(2-thienyl)-L-alanyl-L-seryl-D-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl-L-(2alpha,3abeta,7abeta)-octahydro-1H-indole-2-carbonyl-;

Custom Peptide Synthesis
cGMP Peptide
  • Registration of APIs
  • CMC information required for an IND
  • IND and NDA support
  • Drug master files (DMF) filing
M.F/Formula
C59H89N19O13S
M.W/Mr.
1304.5
Sequence
One Letter Code:RRPXGXSXXR
Three Letter Code:H-D-Arg-Arg-Pro-Hyp-Gly-2Thi-Ser-D-Tic-Oic-Arg-OH
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
InChI
InChI=1S/C59H89N19O13S/c60-37(14-5-19-67-57(61)62)48(82)72-38(15-6-20-68-58(63)64)52(86)75-22-8-18-43(75)54(88)77-30-35(80)26-44(77)50(84)70-28-47(81)71-40(27-36-13-9-23-92-36)49(83)74-41(31-79)53(87)76-29-34-12-2-1-10-32(34)24-46(76)55(89)78-42-17-4-3-11-33(42)25-45(78)51(85)73-39(56(90)91)16-7-21-69-59(65)66/h1-2,9-10,12-13,23,33,35,37-46,79-80H,3-8,11,14-22,24-31,60H2,(H,70,84)(H,71,81)(H,72,82)(H,73,85)(H,74,83)(H,90,91)(H4,61,62,67)(H4,63,64,68)(H4,65,66,69)/t33-,35+,37+,38-,39-,40-,41-,42-,43-,44-,45-,46+/m0/s1
InChI Key
QURWXBZNHXJZBE-SKXRKSCCSA-N
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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