Desformylflustrabromine hydrochloride

Product Description

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

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