Desformylflustrabromine hydrochloride
(Synonyms: Deformylflustrabromine hydrochloride; dFBr hydrochloride) 目录号 : GC12593
Desformylflustrabromine hydrochloride 是 α4β2 神经元烟碱乙酰胆碱受体 (nAChR) 的选择性激动剂，pEC50 为 6.48。
Cas No.:951322-11-5
Sample solution is provided at 25 µL, 10mM.
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Desformylflustrabromine hydrochloride is a selective agonist of α4β2 neuronal nicotinic acetylcholine receptor (nAChR) with a pEC50 of 6.48.
Desformylflustrabromine hydrochloride is a selective agonist of α4β2 neuronal nicotinic acetylcholine receptor (nAChR) with a pEC50 of 6.48[1]. ACh-induced currents are potentiated and inhibited by Desformylflustrabromine hydrochloride in the high sensitivity (HS) and low sensitivity (LS) isoform preparations, although Desformylflustrabromine hydrochloride displays a higher potency on the LS isoform (pEC50=6.4±0.2) compare with the HS isoform (pEC50=5.6±0.2). Desformylflustrabromine hydrochloride potentiates ACh-induced responses of wild-type receptors expressed using the HS isoform preparation maximally by 350±20%, which is similar to receptors expressed via the LS isoform preparation (350±30%)[2].
References:
[1]. Nadezhda German, et al. Deconstruction of the α4β2 Nicotinic Acetylchloine (nACh) Receptor Positive Allosteric Modulator des-Formylflustrabromine (dFBr). J Med Chem. 2011 Oct 27;54(20):7259-67.
[2]. Weltzin MM, et al. Desformylflustrabromine Modulates α4β2 Neuronal Nicotinic Acetylcholine Receptor High- and Low-Sensitivity Isoforms at Allosteric Clefts Containing the β2 Subunit. J Pharmacol Exp Ther. 2015 Aug;354(2):184-94.
Kinase experiment: | Receptors expressed via the high sensitivity (HS) isoform preparation are evaluated for Desformylflustrabromine hydrochloride modulation by coapplication of 10 μM ACh with increasing concentrations of Desformylflustrabromine hydrochloride (0.001 to 100 μM). To compare responses from different oocytes, individual responses to Desformylflustrabromine hydrochloride application are normalized to the control responses elicited using either 10 or 100 μM ACh for receptors expressed by the HS or LS isoform preparations, respectively, for both wild-type and mutated receptors. Data are collected from at least four replicate experiments using oocytes obtained from at least two different frogs[2]. |
References: [1]. Nadezhda German, et al. Deconstruction of the α4β2 Nicotinic Acetylchloine (nACh) Receptor Positive Allosteric Modulator des-Formylflustrabromine (dFBr). J Med Chem. 2011 Oct 27;54(20):7259-67. | |
| Cas No. | 951322-11-5 | SDF | |
| 别名 | Deformylflustrabromine hydrochloride; dFBr hydrochloride | ||
| 化学名 | 2-(6-bromo-2-(2-methylbut-3-en-2-yl)-1H-indol-3-yl)-N-methylethanamine hydrochloride | ||
| Canonical SMILES | BrC1=CC=C2C(CCNC)=C(C(C)(C=C)C)NC2=C1.Cl | ||
| 分子式 | C16H21BrN2.HCl | 分子量 | 357.72 |
| 溶解度 | DMSO : ≥ 105 mg/mL (293.53 mM); H2O : 5 mg/mL (13.98 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7955 mL | 13.9774 mL | 27.9548 mL |
| 5 mM | 0.5591 mL | 2.7955 mL | 5.591 mL |
| 10 mM | 0.2795 mL | 1.3977 mL | 2.7955 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet