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Luzindole Sale

(Synonyms: N-乙酰-2-苄基色胺,N-0774) 目录号 : GC17898

A melatonin receptor antagonist

Luzindole Chemical Structure

Cas No.:117946-91-5

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥2,200.00
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1mg
¥684.00
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5mg
¥1,710.00
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10mg
¥2,790.00
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Sample solution is provided at 25 µL, 10mM.

Description

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).

化学性质

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
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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。
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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
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