| 货号 | 3328/50 |
| 别名 | 6-Bromo-2-(1,1-dimethyl-2-propenyl) |
| 供应商 | Tocris |
| 生物活性 | 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. |
| 运输条件 | Blue Ice |
| 存放说明 | 4℃ |
| 纯度 | >98 % |
| 计算分子量 | 357.72 |
| 分子式 | C16H21BrN2.HCl |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO and to 10 mM in water with gentle warming |
| CAS号 | 474657-72-2 |
| 参考文献 | Hamoudaet al (2015) Desformylflustrabromine (dFBr) and [3H]dFBr-labeled binding sites in a nicotinic acetylcholine receptor. Mol.Pharmacol. 88 1. PMID: 25870334. 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. 334917. Kimet al (2007) Synthesis of desformylflustrabromine and its evaluation as an α4β2 and α7 nACh receptor modulator. Bioorg.Med.Chem.Lett. 17 4855. PMID: 17604168. Salaet al (2005) Potentiation of human α4β2 neuronal nicotinic receptors by a Flustra foliacea metabolite. Neurosci.Lett. 37344. |