Icatibant Acetate (HOE 140)
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-L-arginine Acetate Salt; 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-(2α,3aβ,7aβ)-octahydro-1H-indole-2-carbonyl-L-arginine Acetate Salt; Firazyr; HOE 140
Icatibant Acetate is a bradykinin B2 receptor antagonist that has been recently approved for treatment of acute attacks of hereditary angioedema (HAE). Icatibant is a synthetic peptide antagonist of the bradykinin B2 receptor with IC50 and Ki values of 1.07 and 0.798nM, respectively, in guinea pig ileal cell membranes.1 It inhibits bradykinin-induced contractions in isolated guinea pig ileum and pulmonary arteries as well as in rat uterus (IC50s = 11, 5.4, and 4.9nM, respectively). In vivo, icatibant inhibits bronchoconstriction induced by bradykinin in a guinea pig model (ID50s = 13.4 and 31.8pmol/kg, i.v., for pulmonary resistance and dynamic lung compliance, respectively).1 Icatibant (30ug, i.v.) also reduces vascular permeability in the footpad and intestine in a mouse model of hereditary angioedema.2 Formulations containing icatibant have been used for the treatment of hereditary angioedema.
Synonyms
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-L-arginine Acetate Salt; 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-(2α,3aβ,7aβ)-octahydro-1H-indole-2-carbonyl-L-arginine Acetate Salt; Firazyr; HOE 140
Molecular Formula
C₅₉H₈₉N₁₉O₁₃S x(C ₂H₄O₂)
Solubility
DMSO (Slightly), Water (Slightly)
Storage and Stability
May be stored at -20°C. Stable for 6 months after receipt at -20°C. Reconstitute with solvent. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Store under inert atmosphere
Important Note
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
Toxicity and Hazards: All products should be handled by qualified personnel only, trained in laboratory procedures.
Important Note
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
