Cat. No. 3978
Biological ActivityPeptide antagonist of the B2 bradykinin receptor (pKi = 10.3); conformationally constrained cyclized analog of HOE 140 (Cat. No. 3014). Blocks hypotension and bronchoconstriction in vivo. Displays selectivity for B2 over 29 other receptors and ion channels (pIC50 < 5.5).
(Modifications: Arg-1 = D-Arg, X-1 = Hyp, X-2 = Thi, X-3 = Dab, X-4 = D-Tic, X-5 = Oic, cyclized 7γ - 10α)
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
Meini et al (1999) MEN 11270, a novel selective constrained peptide antagonist with high affinity at the human B2 kinin receptor. J.Pharmacol.Exp.Ther. 289 1250. PMID: 10336513.
Tramontana et al (2001) Differences between peptide and nonpeptide B2 bradykinin receptor antagonists in blocking bronchoconstriction and hypotension induced by bradykinin in anesthetized guinea pigs J.Pharmacol.Exp.Ther. 296 1051. PMID: 11181940.
Cucchi et al (2002) Interaction of linear and cyclic peptide antagonists at the human B(2) kinin receptor. Peptides 23 1457. PMID: 12182947.
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Keywords: MEN 11270, supplier, MEN11270, analog, icatibant, HOE, 140, HOE140, b2, bradykinin, receptor, antagonist
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