Biological Activity
Peptide 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).
Technical Data
| M. Wt | 1299.56 |
| Formula | C60H90N20O11S |
| Sequence |
RRPXGXXXXR (Modifications: Arg-1 = D-Arg, X-1 = Hyp, X-2 = Thi, X-3 = Dab, X-4 = D-Tic, X-5 = Oic, cyclized 7γ - 10α) |
| Storage | Store at -20°C |
| CAS Number | 235082-52-7 |
| PubChem ID | 90488898 |
| InChI Key | LPLBKEKLEUYDEJ-UUHVOKIZSA-N |
| Smiles | [H]N[C@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1CCC[C@H]1C(=O)N1C[C@H](O)C[C@H]1C(=O)NCC(=O)N[C@H](CC1=CC=CS1)C(=O)N[C@H]1CCNC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H]2CC3CCCCC3N2C(=O)[C@H]2CC3=CC=CC=C3CN2C1=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 1 mg/ml in 30% acetonitrile / water |
Preparing Stock Solutions
The following data is based on the product molecular weight 1299.56. 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 | 0.77 mL | 3.85 mL | 7.69 mL |
| 5 mM | 0.15 mL | 0.77 mL | 1.54 mL |
| 10 mM | 0.08 mL | 0.38 mL | 0.77 mL |
| 50 mM | 0.02 mL | 0.08 mL | 0.15 mL |
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References
References are publications that support the products' biological activity.
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
Keywords: MEN 11270, supplier, MEN11270, analog, icatibant, HOE, 140, HOE140, b2, bradykinin, receptor, antagonist, Bradykinin, Receptors, Bradykinin, Receptors, Tocris Bioscience
