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Submit ReviewDesformylflustrabromine hydrochloride
Description: Positive allosteric modulator of α4β2 nAChRs; also muscle-type nAChR inhibitor
Chemical Name: 6-Bromo-2-(1,1-dimethyl-2-propenyl)-N-1H-indole-3-ethanamine hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for Desformylflustrabromine hydrochloride
Desformylflustrabromine hydrochloride is a 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 for Desformylflustrabromine hydrochloride
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Desformylflustrabromine hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 35.77 | 100 | |
| water | 3.58 | 10 with gentle warming |
Preparing Stock Solutions for Desformylflustrabromine hydrochloride
The following data is based on the product molecular weight 357.72. Batch specific molecular weights may vary from batch to batch due to the degree 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 for Desformylflustrabromine hydrochloride
References for Desformylflustrabromine hydrochloride
References are publications that support the biological activity of the product.
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
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
Hamouda et al (2015) Desformylflustrabromine (dFBr) and [3H]dFBr-labeled binding sites in a nicotinic acetylcholine receptor. Mol.Pharmacol. 88 1 PMID: 25870334
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Literature in this Area
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Nicotinic ACh Receptors Scientific Review
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