Luzindole
(Synonyms: N-乙酰-2-苄基色胺,N-0774) 目录号 : GC17898
A melatonin receptor antagonist
Cas No.:117946-91-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
In addition to intrinsic antioxidant activities, melatonin evokes its effects through the G protein-coupled receptors MT1A (MT1) and MT1B (MT2).[1] Luzindole is a melatonin receptor antagonist that preferentially targets MT1B over MT1A (Ki values are = 10-27 and 158-513 nM, respectively).[2],[3],[4] Luzindole is used both in vitro and in vivo to evaluate the roles of melatonin receptor signaling in diverse pathways, including circadian rhythms, animal behavior, and melanophore response.[5],[6],[2]
Reference:
[1]. Chan, K.H., and Wong, Y.H. A molecular and chemical perspective in defining melatonin receptor subtype selectivity. International Journal of Molecular Sciences 14(9), 18385-18406 (2013).
[2]. Teh, M.T., and Sugden, D. Comparison of the structure-activity relationships of melatonin receptor agonists and antagonists: Lengthening the N-acyl side-chain has differing effects on potency on Xenopus melanophores. Naunyn-Schmiedeberg's Archives of Pharmacology 358(5), 522-528 (1998).
[3]. Dubocovich, M.L. Luzindole (N-0774): A novel melatonin receptor antagonist. Journal of Pharmacology and Experimental Therapeutics 246(3), 902-910 (1988).
[4]. Dubocovich, M.L., Masana, M.I., Iacob, S., et al. Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor. Naunyn-Schmiedeberg's Arch. Pharmacol. 355(3), 365-375 (1997).
[5]. Dubocovich, M.L., Yun, K., Al-Ghoul, W.M., et al. Selective MT2 melatonin receptor antagonists block melatonin-mediated phase advances of circadian rhythms. The FASEB Journal 12(12), 1211-1220 (1998).
[6]. Laredo, S.A., Orr, V.N., McMackin, M.Z., et al. The effects of exogenous melatonin and melatonin receptor blockade on aggression and estrogen-dependent gene expression in male California mice (Peromyscus californicus). Physiology & Behavior 128, 86-91 (2014).
| Cas No. | 117946-91-5 | SDF | |
| 别名 | N-乙酰-2-苄基色胺,N-0774 | ||
| 化学名 | N-(2-(2-benzyl-1H-indol-3-yl)ethyl)acetamide | ||
| Canonical SMILES | O=C(C)NCCC1=C(CC2=CC=CC=C2)NC3=CC=CC=C13 | ||
| 分子式 | C19H20N2O | 分子量 | 292.38 |
| 溶解度 | 20mg/mL in DMSO, 30mg/mL in DMF, 30mg/mL in Ethanol | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.4202 mL | 17.101 mL | 34.2021 mL |
| 5 mM | 0.684 mL | 3.4202 mL | 6.8404 mL |
| 10 mM | 0.342 mL | 1.7101 mL | 3.4202 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。