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.
All Tocris products are intended for laboratory research use only.
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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