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) |
| Storage | Desiccate at -20°C |
| CAS Number | 229030-05-1 |
| PubChem ID | 10374059 |
| InChI Key | STDZHNYUPODPLD-DDLDLQAOSA-N |
| Smiles | CC[C@H](C)[C@H](NC(=O)[C@@H](CC1=CC2=CC=CC=C2C=C1)NC(=O)[C@H](CO)NC(=O)[C@](C)(CC1=CC=CC=C1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCCN)NC(C)=O)C(O)=O |
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.
Solubility Data
| Solubility | Soluble to 2 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 1154.37. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.87 mL | 4.33 mL | 8.66 mL |
| 5 mM | 0.17 mL | 0.87 mL | 1.73 mL |
| 10 mM | 0.09 mL | 0.43 mL | 0.87 mL |
| 50 mM | 0.02 mL | 0.09 mL | 0.17 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Gobeil et al (1996) Structure-activity studies of B1 receptor related peptide. Hypertension 28 833 PMID: 8901831
Duka et al (2003) Mechanisms mediating the vasoactive effects of the B1 receptors of bradykinin. Hypertension 42 1021 PMID: 14557281
Gobeil et al (1998) Kinin B1 receptor antagonists containing α-methyl-L-phenylalanine: in vitro and in vivo antagonistic activities. Hypertension 33 823 PMID:
Keywords: R 892, supplier, Potent, selective, B1, antagonists, Receptors, Bradykinin, R892, Bradykinin, Receptors, Bradykinin, Receptors, Tocris Bioscience
