A 582941
目录号 : GC17805A 582941 是 α7 nAChR 的有效、选择性和脑穿透性部分激动剂,在大鼠脑膜和人类额叶皮层中的 Kis 分别为 10.8 和 16.7 nM。
Cas No.:848591-90-2
Sample solution is provided at 25 µL, 10mM.
A 582941 is a highly selective partial agonist of α7 nicotinic acetylcholine receptors (nAChRs), with an EC50 value of 4260 nM to human α7 nAChRs [1].
nAChRs are a family of pentameric ligand-gated ion channels. They are derived from multiple α (α2-α10) and β (β2-β4) subunit genes. α7 nAChR receptor exhibits higher Ca2+ permeability than other nAChR combinations. These receptors modulate the release of multiple neurotransmitters, including acetylcholine (ACh), glutamate, and GABA [1].
In FLIPR, A 582941 did not activate recombinant heteromeric nAChRs (α4β2, α3β2, α3β4, or α4β4) according to Ca2+ dynamics results. In IMR-32 cells expressing native human α3β4 nAChRs, A 582941 did not produce an agonist effect (with an efficacy less than 20% at concentrations up to 100,000 nM). In Xenopus oocytes expressing an α9α10 nAChR construct, A 582941 at concentrations up to 100,000 nM did not evoke currents. With respect to nAChRs, A 582941 activated only the homomeric α7 subtype [1].
In a rat model of short-term memory based on olfactory cues, saline-treated adults used investigation times during the second session nearly equal to the first session, exhibiting little recognition of the juvenile. Treatment with A 582941 in adult rats resulted in a dose-related reduction in the exploration time during the second session compared with the first session, exhibiting improved recognition of the juvenile [1].
Reference:
[1]. Tietje KR, Anderson DJ, Bitner RS, et al. Preclinical Characterization of A-582941: A Novel α7 Neuronal Nicotinic Receptor Agonist with Broad Spectrum Cognition-Enhancing Properties. CNS neuroscience & therapeutics, 2008, 14(1): 65-82.
Cas No. | 848591-90-2 | SDF | |
化学名 | (3aR,6aR)-2-methyl-5-(6-phenylpyridazin-3-yl)octahydropyrrolo[3,4-c]pyrrole | ||
Canonical SMILES | CN1C[C@H]2[C@@H](CN(C3=NN=C(C4=CC=CC=C4)C=C3)C2)C1 | ||
分子式 | C17H20N4 | 分子量 | 280.37 |
溶解度 | <28.04mg/ml in DMSO; <14.02mg/ml in 1eq. HCl | 储存条件 | Desiccate at RT |
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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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.5667 mL | 17.8336 mL | 35.6672 mL |
5 mM | 0.7133 mL | 3.5667 mL | 7.1334 mL |
10 mM | 0.3567 mL | 1.7834 mL | 3.5667 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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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。
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