BTS 54-505 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.
IC50:去甲肾上腺素吸收的IC50为0.066 μM;对5-HT摄取的IC50为5.1 μM;多巴胺摄取的IC50为 0.31 μM.
西布曲明盐酸(BTS 54-524)是单胺再摄取的抑制剂,在啮齿动物中具有公认的非三环类抗抑郁活性.BTS 54-505是西布曲明的伯胺代谢物.
体外实验:BTS 54-505与5-HT同时给药,延长了5-HT介导的放电活动抑制的恢复时间.BTS 54-505延长了NA-介导的放电活动增强的恢复时间.BTS 54-505对恢复时间的影响归因于对5-HT和NA摄取的抑制.与BTS 54-505的共注射不影响5-HT或NA的应答幅度[1].
在体实验:西布曲明盐酸的仲胺代谢物BTS 54-354和伯胺代谢物BTS 54-505与母体化合物具有相似的体内药理活性.因此,在急性行为模型中,每个化合物具有有效的活性和抗抑郁作用,对于单胺吸收的抑制效果相当[2].
临床试验:截至目前,BTS 54-505仍处于临床前开发阶段.
参考文献:
[1] Scott G, Luscombe GP, Mason R. The effects of BTS 54-505, a metabolite of sibutramine, on monoamine and excitatory amino acid-evoked responses in the rat dorsolateral geniculate nucleus in vivo. Br J Pharmacol. 1994 Jan;111(1):97-102.
[2] Luscombe GP, Hopcroft RH, Thomas PC, Buckett WR. The contribution of metabolites to the rapid and potent down-regulation of rat cortical beta-adrenoceptors by the putative antidepressant sibutramine hydrochloride. Neuropharmacology. 1989 Feb;28(2):129-34.
Physical Appearance | White solid |
Storage | Desiccate at RT |
M.Wt | 288.26 |
Cas No. | 84484-78-6 |
Formula | C15H22NCl·HCl |
Solubility | <28.83mg/ml in DMSO; <14.41mg/ml in H2O |
Chemical Name | (R)-1-(1-(4-chlorophenyl)cyclobutyl)-3-methylbutan-1-amine hydrochloride |
SDF | Download SDF |
Canonical SMILES | ClC1=CC=C(C=C1)C2([C@@H](CC(C)C)N)CCC2.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。 |