Biological Activity
Potent and selective bradykinin B1 receptor antagonist (pA2 = 8.49). Displays no activity at B2 receptors. Reduces mechanical hypernociception in a mouse model of neuropathic pain. Metabolically stable.
Technical Data
| M. Wt | 1140.35 |
| Formula | C57H81N13O12 |
| Sequence |
KRPPGFSXI (Modifications: Lys-1 = N-terminal Ac, X = DβNal) |
| Storage | Desiccate at -20°C |
| CAS Number | 185052-09-9 |
| PubChem ID | 5311397 |
| InChI Key | DOSXOGUJJBDRGQ-VUBDHFCFSA-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@H](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 5 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 1140.35. 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 | 0.88 mL | 4.38 mL | 8.77 mL |
| 5 mM | 0.18 mL | 0.88 mL | 1.75 mL |
| 10 mM | 0.09 mL | 0.44 mL | 0.88 mL |
| 50 mM | 0.02 mL | 0.09 mL | 0.18 mL |
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References
References are publications that support the products' biological activity.
Gobeil et al (1996) Structure-activity studies of B1 receptor-related peptides. Hypertension. 28 833 PMID: 8901831
Quintao et al (2008) Neuropathic pain-like behavior after brachial plexus avulsion in mice: the relevance of kinin B1 and B2 receptors. J.Neurosci. 28 2856 PMID: 18337416
Abdouh et al (2008) Retinal plasma extravasation in streptozotocin-diabetic rats mediated by kinin B1 and B2 receptors. Br.J.Pharmacol. 154 136 PMID: 18311190
Keywords: R 715, supplier, Potent, selective, B1, antagonists, Receptors, Bradykinin, R715, Bradykinin, Receptors, Bradykinin, Receptors, Tocris Bioscience
