Biological Activity
Positive allosteric modulator of nicotinic α4β2 receptors; selectively increases the ionic current through α4β2 in the presence of ACh. Displays 14.7-fold selectivity for α4β2 over homomeric (α7) receptors. Moderately cytotoxic in HCT-116 cells. Also inhibits human muscle (αβεδ) and Torpedo (αβγδ) nAChRs (IC50 values are 1.0 and 0.1 μM, respectively) by binding in the ion channel.
Technical Data
| M. Wt | 357.72 |
| Formula | C16H21BrN2.HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 951322-11-5 |
| PubChem ID | 56675778 |
| InChI Key | GEZWEAPBLKXKGN-UHFFFAOYSA-N |
| Smiles | CNCCC2=C(C(C)(C)C=C)NC1=CC(Br)=CC=C12.Cl |
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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 35.77 | 100 | |
| water | 3.58 | 10mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 357.72. 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 | 2.8 mL | 13.98 mL | 27.95 mL |
| 5 mM | 0.56 mL | 2.8 mL | 5.59 mL |
| 10 mM | 0.28 mL | 1.4 mL | 2.8 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Kim et al (2007) Synthesis of desformylflustrabromine and its evaluation as an α4β2 and α7 nACh receptor modulator. Bioorg.Med.Chem.Lett. 17 4855 PMID: 17604168
Sala et al (2005) Potentiation of human α4β2 neuronal nicotinic receptors by a Flustra foliacea metabolite. Neurosci.Lett. 373 44 PMID:
Weltzin and Schulte (2010) Pharmacological characterization of the allosteric modulator desformylflustrabromine and its interaction with α4β2 neuronal nicotinic acetylcholine receptor orthosteric ligands. J.Pharm.Exp.Ther. 334 917 PMID:
Hamouda et al (2015) Desformylflustrabromine (dFBr) and [3H]dFBr-labeled binding sites in a nicotinic acetylcholine receptor. Mol.Pharmacol. 88 1 PMID: 25870334
Keywords: Desformylflustrabromine hydrochloride, supplier, dFBr, a4b2, nicotinic, acetylcholine, receptor, receptors, nAChR, positive, allosteric, modulators, Nicotinic, (a4b2), Receptors, Nicotinic, Receptors, (Other, Subtypes), Nicotinic, (a4b2), Receptors, Tocris Bioscience
