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R 892

Cat. No. 3226

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Biological Activity

Potent and selective bradykinin B₁ receptor antagonist (ID₅₀ values are 2.8 and > 600 nM at B₁ and B₂ receptors respectively). Exhibits no intrinsic agonist activity and is resistant to aminopeptidase and kininase II (ACE) cleavage. Displays hypertensive activity in vivo.

Technical Data

M.Wt:

1154.37

Formula:

C₅₈H₈₃N₁₃O₁₂

Sequence:

KRPPGFSXI

(Modifications: Lys-1 = N-terminal Ac, Phe-6 = (αMe)Phe, X = DβNal)

Solubility:

Soluble to 5 mg/ml in water

Storage:

Desiccate at -20°C

CAS No:

229030-05-1

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

Gobeil et al (1996) Structure-activity studies of B₁ receptor related peptide. Hypertension 28 833. PMID: 8901831.

Gobeil et al (1998) Kinin B₁ receptor antagonists containing α-methyl-L-phenylalanine: in vitro and in vivo antagonistic activities. Hypertension 33 823.

Duka et al (2003) Mechanisms mediating the vasoactive effects of the B₁ receptors of bradykinin. Hypertension 42 1021. PMID: 14557281.

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Keywords: R 892, supplier, Potent, selective, B1, antagonists, Receptors, Bradykinin, R892

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