Biological Activity
Potent bombesin receptor subtype 3 (BRS-3; BB3) agonist (IC50 = 2.52 nM). Also GRPR (BB1) and NMBR (BB2) agonist (IC50 values are 0.26 and 1.55 nM respectively). Enhances glucose transport in obese and diabetic primary myocytes. Also stimulates NCI-H1299 lung cancer cell proliferation in vitro.
Technical Data
| M. Wt | 1133.32 |
| Formula | C57H76N14O11 |
| Sequence |
YQWAVAHFX (Modifications: Tyr-1= D-Tyr, Ala-6 = β-Ala, X = Nle, Nle-9 = C-terminal amide) |
| Storage | Store at -20°C |
| CAS Number | 183241-31-8 |
| PubChem ID | 91826107 |
| InChI Key | BXSSCSKCOFKPOK-ZWAOGYCRSA-N |
| Smiles | [H]N[C@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CCCC)C(N)=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 1133.32. 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 | 4.41 mL | 8.82 mL |
| 5 mM | 0.18 mL | 0.88 mL | 1.76 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.
González et al (2015) Effect of bombesin receptor subtype-3 and its synthetic agonist on signaling, glucose transport and metabolism in myocytes from patients with obesity and type 2 diabetes Int.J.Mol.Med. 35 925 PMID: 25653074
Moody et al (2015) ML-18 is a non-peptide bombesin receptor subtype-3 antagonist which inhibits lung cancer growth. Peptides 64 55 PMID: 25554218
Moreno et al (2013) Comparative pharmacology of bombesin receptor subtype-3, nonpeptide agonist MK-5046, a universal peptide agonist, and peptide antagonist Bantag-1 for human bombesin receptors. J.Pharmacol.Exp.Ther. 347 100 PMID: 23892571
Mantey et al (1997) Discovery of a high affinity radioligand for the human orphan receptor, bombesin receptor subtype 3, which demonstrates that it has a unique pharmacology compared with other mammalian bombesin receptors. J Biol Chem. 272 26062 PMID: 9325344
Keywords: BA 1, supplier, BA1, bombesin, receptors, subtype3, BRS3, BB3, BB1, BB2, neuromedinB, NMBR, GRPR, gastrin-releasing, peptides, hormones, Bombesin, Receptors, Bombesin, Receptors, Tocris Bioscience
