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Icatibant

Icatibant Struktur
130308-48-4
CAS-Nr.
130308-48-4
Englisch Name:
Icatibant
Synonyma:
H-D-ARG-ARG-PRO-HYP-GLY-THI-SER-D-TIC-OIC-ARG-OH;S-0765;H0E-140;HOE I40;HOE 140;JE-049);Etibant;Icatibant;HOE 140 TFA;Icatibant [inn]
CBNumber:
CB1318492
Summenformel:
C59H89N19O13S
Molgewicht:
1304.52
MOL-Datei:
130308-48-4.mol

Icatibant Eigenschaften

Dichte
1.60±0.1 g/cm3(Predicted)
storage temp. 
Sealed in dry,2-8°C
L?slichkeit
Water:100.0(Max Conc. mg/mL);76.66(Max Conc. mM)
Aggregatzustand
powder
pka
3.60±0.21(Predicted)
Farbe
white
Wasserl?slichkeit
Soluble to 1 mg/ml in water
Sequenz
H-D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Tic-Oic-Arg-OH
InChIKey
QASONHYHOCRAHL-DOMVFXHKSA-N
CAS Datenbank
130308-48-4

Sicherheit

WGK Germany  3

Icatibant Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Hoe 140 (D-Arg-[Hyp3, Thi5, D-Tic7, Oic8]-bradykinin), on bradykinin- and platelet-activating factor (PAF)-induced bronchoconstriction and airway microvascular leakage in anesthetized guinea pigs. Hoe 140 is highly potent and long-acting in inhibiting BK-induced hypotensive responses in the rat. Four hours after s.c. administration of 20nmol kg-1, inhibition still amounted to 60% whereas the effect of 200nmol kg-1 of d-Arg-[Hyp2, Thi5,8, d-Phe7]BK was not significant[1-2].

History

Icatibant, developed by Germany's Jerini AG (which was acquired by Shire in 2008 and subsequently by Takeda), is a specific bradykinin B2 receptor antagonist used to treat acute episodes of hereditary angioedema. It works by inhibiting the effects of bradykinin, which is associated with localized swelling, inflammation, and pain. First approved in the European Union in 2008 under the trade name Firazyr for the treatment of acute HAE attacks in adults, it received accelerated approval from the FDA in 2011 via priority review for acute HAE attacks in patients aged 18 years and older. In 2017, the European Union further expanded its approved indications to include pediatric and adolescent HAE patients aged 2 years and above.
Icatibant

Verwenden

Icatibant is an antagonist of the human bradykinin B2 receptor (B2R), that can be used for the treatment of hereditary angioedema (HAE). Upon administration, icatibant targets and binds to B2R, thereby preventing bradykinin from binding to the B2R. This may prevent bradykinin/B2R-mediated vasodilation, the resulting increase in vascular permeability, and the swelling, inflammation, and pain associated with HAE. This may also prevent or improve pulmonary edema not associated with HAE and improve the associated decrease in blood oxygen levels.

Definition

ChEBI: Icatibant is a ten-membered synthetic oligopeptide consisting of D-Arg, Arg, Pro, Hyp, Gly, Thi, Ser, D-Tic, Oic, and Arg residues joined in sequrence. A bradykinin receptor antagonist used as its acetate salt for the treatment of acut attacks of hereditary angioedema in adult patients.

Trademarks

Metastat (CollaGenex).

Biologische Aktivit?t

Hoe 140 is highly potent and long-acting in inhibiting BK-induced hypotensive responses in the rat. Four hours after s.c. administration of 20 nmol kg1, inhibition still amounted to 60%, whereas the effect of 200 nmol kg1 of d-Arg—[Hyp2, Thi5,8, d-Phe7]BK was not significant. In receptor binding studies in guinea-pig ileum preparations, Hoe 140 showed an IC50 of 1.07 × 109mol l1 and a KI value of 7.98 × 1010 mol l1.

Icatibant Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Icatibant Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 158)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795
ivan@atkchemical.com China 33024 60
Shenzhen Nexconn Pharmatechs Ltd
+86-755-89396905 +86-15013857715
admin@nexconn.com China 10403 58
Jinan Carbotang Biotech Co.,Ltd.
+8615866703830
figo.gao@foxmail.com China 8497 58
Beijing Yibai Biotechnology Co., Ltd
0086-182-6772-3597
sales04@yibaibiotech.com CHINA 419 58
CONIER CHEM AND PHARMA LIMITED
+8618523575427
sales@conier.com China 49979 58
career henan chemical co
+86-0371-86658258 +8613203830695
factory@coreychem.com China 29792 58
Zhengzhou Alfa Chemical Co.,Ltd
+8618530059196
sale04@alfachem.cn China 9544 58
Hebei Yanxi Chemical Co., Ltd.
+8618531123677
faithe@yan-xi.com China 5853 58
TargetMol Chemicals Inc.
+1-781-999-5354; +17819995354
marketing@targetmol.com United States 32467 58
Hubei Ipure Biology Co., Ltd
+8613367258412
ada@ipurechemical.com China 10236 58

130308-48-4()Verwandte Suche:


  • RRP-(HYP)-G-(THI)-S-(D-TIC)-(OIC)-R
  • H2N-D-ARG-ARG-PRO-HYP-GLY-THI-SER-D-TIC-OIC-ARG-OH
  • Icatibant
  • D-Arg-[Hyp3,Thi5,D-Tic7,Oic8]bradykinin
  • D-Arg-L-Arg-L-Pro-L-t4Hyp-Gly-L-Thi-L-Ser-D-Tic-L-Oic-L-Arg-OH
  • H0E-140
  • D-Arg-L-Arg-L-Pro-L-t4Hyp-Gly-3-(2-Thienyl)-L-Ala-L-Ser-D-Tic-[(3aS,7aS)-L-Oic-]-OH
  • Des-Arg9-D-Arg[Hyp3,Thi5,D-Tic7,Oic8]bradykinin
  • S-0765
  • Icatibant [inn]
  • 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-
  • HOE I40
  • HOE 140
  • HOE 140 2ACOH 4H2O
  • D-ARG-ARG-PRO-HYP-GLY-THI-SER-D-TIC-OIC-ARG
  • D-ARG-ARG-PRO-HYP-GLY-THI-SER-D-TIC-OIC-ARG 2ACOH 4H2O
  • D-ARGINYL-[HYP3,THI5,D-TIC7,OIC8]-BRADYKININ
  • D-ARGINYL-[HYP3,THI5,D-TIC7,OIC8]-BRADYKININ 2ACOH 4H2O
  • D-ARGINYL-L-ARGINLYL-L-PROLYL-TRANS-4-HYDROXY-L-PROLYLGLYCYL-3-(2-THIENYL)-L-ALANYL-L-SERYL-D-1,2,3,4-TETRAHYDRO-3-ISOQUINOLINECARBONYL-L-(2ALPHA, 3BETA, 7ABETA)-OCTAHYDRO-1H-INDOLE-2-CARBONYL
  • D-ARGINYL-L-ARGINLYL-L-PROLYL-TRANS-4-HYDROXY-L-PROLYLGLYCYL-3-(2-THIENYL)-L-ALANYL-L-SERYL-D-1,2,3,4-TETRAHYDRO-3-ISOQUINOLINECARBONYL-L-(2ALPHA,3BETA,7A-BETA)-OCTAHYDRO-1H-INDOLE-2-CARBONYL-L-ARGININE
  • [DES-ARG10] HOE 140
  • D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Tic-Oic
  • D-Arg-L-Arg-L-prolyl-L-Hyp-Gly-L-(2-thienyl)Ala-L-Ser-D-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl-L-(2α,3β,7aβ)-octahydro-1H-indole-2-carboxylic acid
  • HOE 140 USP/EP/BP
  • L-Arginine, D-arginyl-L-arginyl-L-prolyl-(4R)-4-hydroxy-L-prolylglycyl-3-(2-thienyl)-L-alanyl-L-seryl-(3R)-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl-(2S,3aS,7aS)-octahydro-1H-indole-2-carbonyl-
  • Nw-(((S)-2-(2-((2S,4R)-1-(D-arginyl-L-arginyl-L-prolyl)-4-hydroxypyrrolidine-2-carboxamido)acetamido)-3-(thiophen-2-yl)propanoyl)-L-seryl)-N2-((3aS,7aS)-octahydro-1H-indole-2-carbonyl)-N2-((R)-1,2,3,4-tetrahydroisoquinoline-3-carbonyl)-L-arginine
  • JE-049)
  • Icatibant (HOE-140
  • Icatibatide Acetate
  • Etibant
  • HOE 140 TFA
  • ((2S,3aS,7aS)-1-((R)-2-(((S)-2-(2-((2S,4R)-1-(D-Arginyl-L-arginyl-L-prolyl)-4-hydroxypyrrolidine-2-carboxamido)acetamido)-3-(thiophen-2-yl)propanoyl)-L-seryl)-1,2,3,4-tetrahydroisoquinoline-3-carbonyl)octahydro-1H-indole-2-carbonyl)-L-arginine
  • Phytol Impurity 3
  • Bradykinin Antagonist, HOE I40 - 1 mg
  • H-D-ARG-ARG-PRO-HYP-GLY-THI-SER-D-TIC-OIC-ARG-OH
  • 130308-48-4
  • C53H77N15O12S
  • C59H90N20O12S
  • peptide
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