Formulation: A crystalline solid
Formal Name: 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
Purity: ≥98%
Formula Markup: C59H89N19O13S • XC2H4O2
Formula Weight: 1304,5
Shelf life (days): 1460
CAS Number: 138614-30-9
Notes: Icatibant is a synthetic peptide antagonist of the bradykinin B2 receptor with IC50 and Ki values of 1.07 and 0.798 nM, respectively, in guinea pig ileal cell membranes.{40794} It inhibits bradykinin-induced contractions in isolated guinea pig ileum and pulmonary arteries as well as in rat uterus (IC50s = 11, 5.4, and 4.9 nM, respectively). In vivo, icatibant inhibits bronchoconstriction induced by bradykinin (Item No. 37408) in a guinea pig model (ID50s = 13.4 and 31.8 pmol/kg, i.v., for pulmonary resistance and dynamic lung compliance, respectively).{40794} Icatibant (30 µg, i.v.) also reduces vascular permeability in the footpad and intestine in a mouse model of hereditary angioedema.{40793} Formulations containing icatibant have been used for the treatment of hereditary angioedema.
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