Desformylflustrabromine hydrochloride

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Cat.No. 3328 - Desformylflustrabromine hydrochloride | C16H21BrN2.HCl | CAS No. 951322-11-5
Description: Positive allosteric modulator of α4β2; also muscle-type nAChR inhibitor
Chemical Name: 6-Bromo-2-(1,1-dimethyl-2-propenyl)-N-1H-indole-3-ethanamine hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

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.

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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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


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Keywords: dFBr a4b2 nicotinic acetylcholine receptor receptors nAChR positive allosteric modulators Nicotinic (a4b2) Receptors

Citations for Desformylflustrabromine hydrochloride

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