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Submit ReviewDesformylflustrabromine hydrochloride
说明： Positive allosteric modulator of α4β2 nAChRs; also muscle-type nAChR inhibitor
化学名： 6-Bromo-2-(1,1-dimethyl-2-propenyl)-N-1H-indole-3-ethanamine hydrochloride
纯度： ≥98% (HPLC)
生物活性 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.
技术数据 for Desformylflustrabromine hydrochloride
| 分子量 | 357.72 |
| 公式 | C16H21BrN2.HCl |
| 储存 | Store at +4°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Desformylflustrabromine hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 35.77 | 100 | |
| water | 3.58 | 10 温和加热 |
制备储备液 for Desformylflustrabromine hydrochloride
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for Desformylflustrabromine hydrochloride
参考文献 for Desformylflustrabromine hydrochloride
参考文献是支持产品生物活性的出版物。
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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关键词: Desformylflustrabromine hydrochloride, Desformylflustrabromine hydrochloride supplier, dFBr, a4b2, nicotinic, acetylcholine, receptor, receptors, nAChR, positive, allosteric, modulators, PAM, Nicotinic, (a4b2), Receptors, (Other, Subtypes), 3328, Tocris Bioscience
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