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Icatibant

CAS No. 130308-48-4

Icatibant( HOE-140 | JE-049 )

Catalog No. M11215 CAS No. 130308-48-4

A selective and specific antagonist of bradykinin B2 receptor (B2R) with IC50 and Ki of 1.07 nM and 0.798 nM respectively.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Icatibant
  • Note
    Research use only, not for human use.
  • Brief Description
    A selective and specific antagonist of bradykinin B2 receptor (B2R) with IC50 and Ki of 1.07 nM and 0.798 nM respectively.
  • Description
    A selective and specific antagonist of bradykinin B2 receptor (B2R) with IC50 and Ki of 1.07 nM and 0.798 nM respectively; protects against memory impairment in mLFPI mice (10 nmol/kg); attenuates the brain edema, interleukin-1β, tumor necrosis factor-α, and nitric oxide metabolites content elicited by mLFPI.Other Indication Approved.
  • In Vitro
    Icatibant (10-30 μM) potentiates angiotensin III, but not angiotensin II (contraction mediated by angiotensin AT1 receptors), and Lys-des-Arg9-bradykinin, but not des-Arg9-bradykinin (effects mediated by the bradykinin B1 receptors).
  • In Vivo
    Icatibant (0.3, or 1.5 mg/kg, subcutaneous administration twice daily in mice) shows a significant preventive effect on ulcerative Colitis. Animal Model:Female mice of the CBA/J (H-2k) strain.Dosage:0.06, 0.3, or 1.5 mg/kg.Administration:Subcutaneous administration twice daily.Result:The length of the large intestine was 93.6±6.8 mm with the 1.5 mg/kg dosage and 94.0±4.1 mm with the 0.3 mg/kg dosage , showing a significant preventive effect on shortening.
  • Synonyms
    HOE-140 | JE-049
  • Pathway
    GPCR/G Protein
  • Target
    Bradykinin Receptor
  • Recptor
    Bradykinin Receptor
  • Research Area
    Other Indications
  • Indication
    Other Disease

Chemical Information

  • CAS Number
    130308-48-4
  • Formula Weight
    1304.522
  • Molecular Formula
    C59H89N19O13S
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    N=C(N)NC(C(C1NCC2=C(C=CC=C2)C1)=O)CC[C@@H](C(O)=O)N(C([C@H](CO)N(C(CN(C([C@H]3N(C([C@H](CCCNC(N)=N)NC([C@@H](CCCNC(N)=N)N)=O)=O)CCC3)=O)C(C4NC[C@H](O)C4)=O)=O)C([C@H](CC5=CC=CS5)N)=O)=O)C(C6N[C@@]7([H])CCCC[C@@]7([H])C6)=O
  • Chemical Name
    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-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Hock FJ, et al. Br J Pharmacol. 1991 Mar;102(3):769-73. 2. Ferreira AP, et al. Psychopharmacology (Berl). 2014 May;231(9):1935-48. 3. Asghar AU, et al. Eur J Pharmacol. 2000 Jun 9;398(1):131-8.
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