A synthetic peptide antagonist of the bradykinin B2 receptor (IC50 = 1.07 nM; Ki = 0.798 nM); inhibits bradykinin-induced contractions in isolated guinea pig ileum and pulmonary arteries as well as in rat uterus (IC50s = 11

Icatibant (acetate) – 5 mg

Brand:
Cayman
CAS:
138614-30-9
Storage:
-20
UN-No:
Non-Hazardous - /

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. 15539) 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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Description

A synthetic peptide antagonist of the bradykinin B2 receptor (IC50 = 1.07 nM; Ki = 0.798 nM); 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); inhibits bradykinin-induced bronchoconstriction in a guinea pig model (ID50s = 13.4 and 31.8 pmol/kg, i.v., for pulmonary resistance and dynamic lung compliance, respectively); reduces vascular permeability in a mouse model of hereditary angioedema (30 µg, i.v.)

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

Synonyms:  HOE 140

Molecular weight: 1,304.50

CAS: 138614-30-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Peptides||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Vasculature|Vasodilation||Research Area|Immunology & Inflammation|Allergy

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