Desformylflustrabromine hydrochloride

Name: Desformylflustrabromine hydrochloride
Brand: Tocris Bioscience
SKU: 3328

Tocris Bioscience, part of Bio-Techne | Catalog # 3328

Citations (5)

COA / SDS

Positive allosteric modulator of α4β2 nAChRs; also muscle-type nAChR inhibitor

Key Product Details

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)
Molecular Weight:	357.72

View Full Technical Details for Desformylflustrabromine hydrochloride

Technical Data
Citations

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 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	2.80 mL	13.98 mL	27.95 mL
5 mM	0.56 mL	2.80 mL	5.59 mL
10 mM	0.28 mL	1.40 mL	2.80 mL
50 mM	0.06 mL	0.28 mL	0.56 mL

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References for Desformylflustrabromine hydrochloride

References are publications that support the biological activity of the product.

Hamouda Desformylflustrabromine (dFBr) and [³H]dFBr-labeled binding sites in a nicotinic acetylcholine receptor. Mol.Pharmacol. 2015 PMID: 25870334
Sala Potentiation of human α4β2 neuronal nicotinic receptors by a Flustra foliacea metabolite. Neurosci.Lett.
Weltzin and Schulte Pharmacological characterization of the allosteric modulator desformylflustrabromine and its interaction with α4β2 neuronal nicotinic acetylcholine receptor orthosteric ligands. J.Pharm.Exp.Ther.
Kim Synthesis of desformylflustrabromine and its evaluation as an α4β2 and α7 nACh receptor modulator. Bioorg.Med.Chem.Lett. 2007 PMID: 17604168