Thiethylperazine dimaleate (Synonyms: 二马来酸硫乙基哌嗪)
目录号: PL12125 纯度: ≥99%
CAS No. :1179-69-7
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中文名称
Thiethylperazine dimaleate
中文别名
马来酸硫乙拉嗪;马来酸乙巯拉嗪;4-硝基吡啶;吩噻嗪-2-(乙硫基)-10-(3-(4-甲基-1-哌嗪基)丙基)-马来酸(1:2);马来酸乙巯拉嗪 USP标准品;马来酸甲哌硫丙嗪;马来酸硫乙哌丙嗪;二马来酸硫乙基哌嗪
英文名称
Thiethylperazine dimaleate
英文别名
Thiethylperazine Maleate;Thiethylperazine Dimaleate;THIETHYLPERAZINE MALEATE (200 MG);THIETHYLPERAZINE MALEATE, USP STANDARD;2-butenedioate;gs-95;Thiethylperazinbishydrogenmaleat;torecan;torecanbimaleate;torecandimaleate;torecanmaleate;toresten;tresten;Thiethylperazine dimaleate
Cas No.
1179-69-7
分子式
C22H29N3S2.C4H4O4
分子量
515.69
包装储存
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
产品详情
Thiethylperazine dimaleate 是一种吩噻嗪衍生物,是一种口服有效的多巴胺 D2 受体和组胺 H1 受体拮抗剂。Thiethylperazine dimaleate 也是一种选择性的 ABCC1 激活剂,可减少小鼠中的淀粉样 β (Aβ) 负荷。Thiethylperazine dimaleate 具有止吐,抗精神病和抗菌作用。
生物活性
Thiethylperazine dimaleate, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine dimaleate is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine dimaleate has anti-emetic, antipsychotic and antimicrobial effects.
性状
Solid
IC50 & Target[1][2]
D2 Receptor H1 Receptor
体外研究(In Vitro)
Thiethylperazine could enhance the antibiotic (Vancomycin) activity at a concentration as low as 2 μg/mL. Thiethylperazine inhibits Vancomycin-sensitive E. faecalis ATCC 29212, Vancomycin-resistant E. faecalis ATCC 51299 and vancomycin-resistant E. faecalis (VREF) isolates with MIC values of 8 μg/mL, 16 μg/mL and 8 μg/mL, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Thiethylperazine (3 mg/kg; intramuscular injection; twice daily; for 30 days; young APP/PS1 mice) treatment significantly reduces Aβ42 levels in APP/PS1 mice. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[1]. Czeizel AE, et al. Case-control study of teratogenic potential of thiethylperazine, an anti-emetic drug. BJOG. 2003 May;110(5):497-9.
[2]. Krohn M, et al. Cerebral amyloid-β proteostasis is regulated by the membrane transport protein ABCC1 in mice. J Clin Invest. 2011 Oct;121(10):3924-31.
[3]. Rahbar M, et al.
溶解度数据
In Vitro: DMSO : 125 mg/mL (197.86 mM; ultrasonic and warming and heat to 60°C)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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