Lu AE58054 Hydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Lu AE58054 Hydrochloride是一种具有体内亲和力和体外选择性的5-HT（6）受体拮抗剂，Ki值为0.83 nM[1]。
血清素6受体（5-HT6R）是14个5- HTRs血清素受体家族中的一员[1]，在与阿尔茨海默氏病和精神分裂症相关联的认知障碍中起重要作用[2]。
在5-HT（6）GTPγS效力实验中，Lu AE58054 Hydrochloride抑制5-HT介导的激活。除了对α（1B）和α（1A）-肾上腺素能受体具有中等亲和力，与其它检测的70多个靶标相比，Lu AE58054 Hydrochloride具有大于50倍的选择性[1]。
在大鼠模型中，口服给药Lu AE58054抑制5-HT 6拮抗剂Lu AE60157的结合，ED50 为2.7 mg/kg。在大鼠中，给予5-20 mg/kg剂量范围的Lu AE58054导致大于65％的5-HT6R结合，逆转phencyclidine造成的认知损害。这些结果表明，Lu AE58054是5- HT6Rs的强效拮抗剂，具有良好的口服生物利用度，对患精神分裂症的大鼠的认知功能障碍具有良好的治疗效果[1]。
参考文献：
[1]. Arnt J, Bang-Andersen B, Grayson B, et al. Lu AE58054, a 5-HT6 antagonist, reverses cognitive impairment induced by subchronic phencyclidine in a novel object recognition test in rats. Int J Neuropsychopharmacol, 2010, 13(8): 1021-1033.
[2]. Witten L, Bang-Andersen B, Nielsen SM, et al. Molecular and Cellular Pharmacology Characterization of [3H]Lu AE60157 ([3H]8-(4-methylpiperazin-1-yl)-3-phenylsulfonylquinoline) binding to 5-hydroxytryptamine6 (5-HT6) receptors in vivo. Eur J Pharmacol, 2012, 676(1-3): 6-11
.| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 434.83 |
| Cas No. | 467458-02-2 |
| Formula | C20H20ClF5N2O |
| Synonyms | Lu AE 58054 Hydrochloride |
| Solubility | ≥21.74 mg/mL in DMSO; ≥3.83 mg/mL in H2O with gentle warming and ultrasonic; ≥51.2 mg/mL in EtOH |
| Chemical Name | 2-(6-fluoro-1H-indol-3-yl)-N-[[3-(2,2,3,3-tetrafluoropropoxy)phenyl]methyl]ethanamine;hydrochloride |
| SDF | Download SDF |
| Canonical SMILES | C1=CC(=CC(=C1)OCC(C(F)F)(F)F)CNCCC2=CNC3=C2C=CC(=C3)F.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
质量控制和MSDS
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化学结构
