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CAS No.: 15421-84-8

Trapidil/唑嘧胺 Catalog No. CSN10166

Synonyms: AR-12008;Trapymin;Avantrin

Trapidil, a vasodilator and an antiplatelet drug, is also a PDGF antagonist that can inhibit the proliferation of the PDGF-producing glioma cells.

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技术信息

生物活性

描述Platelet-derived growth factors (PDGFs) are composed of five kinds of ligand dimers, PDGF-AA, -BB, -AB, -CC, and -DD, which bind to three kinds of their receptor dimmers, PDGF receptor (PDGFR) αα, αβ, and ββ, with different affinities. The PDGFs transduce overlapping but not identical cellular signals, such as Src, JNK, Akt, and PLCγ, for regulating cellular properties, including proliferation and migration. Trapidil is a vasodilator and antiplatelet agent and also a platelet-derived growth factor antagonist. Trapidil at 100 µg/ml significantly inhibited the proliferation of U251MG cells, while there was no inhibitory effect on U105MG cells (which do not produce the PDGF-like molecule)^[3]. Trapidil at 400 μM strongly inhibited osteoclastogenesis in mice by abrogating receptor activator of NF-kB ligand-induced calcium oscillation and Pim-1 expression required for NFATc1 (a master transcription factor for osteoclastogenesis) induction^[4]. It was also fund that trapidil treatment at 100 to 400 μg/ml significantly inhibited human mesangial cell proliferation, which might be related to the inhibition of PDGF-BB binding to its receptors and modulation of PDGFβ-receptor gene expression^[5]. Trapidil at 400 μg/ml inhibited the PDGF-stimulated MAP kinase activation by 35% at 10 minutes and by 32% at 6 hours but had no effect on MAP kinase protein expression levels^[6].
动物研究
剂量
Rabbit: 30 mg/kg^[3] (s.c., BID) Rat: 4 mg/kg, 20 mg/kg^[4] (i.p.), 30 mg/kg - 90 mg/kg^[5] (i.p., lethal dose: 90 mg/kg); 100 mg/kg^[6] (p.o.)

给药途径
s.c., i.p., p.o.
临床研究

动物研究
剂量	Rabbit: 30 mg/kg^[3] (s.c., BID) Rat: 4 mg/kg, 20 mg/kg^[4] (i.p.), 30 mg/kg - 90 mg/kg^[5] (i.p., lethal dose: 90 mg/kg); 100 mg/kg^[6] (p.o.)
给药途径	s.c., i.p., p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00914420	Coronary Artery Disease ... more >> Acute Coronary Syndrome Collapse <<	Phase 4	Unknown	October 2012	Italy ... more >> University Hospital Modena Recruiting Modena, Italy Contact: Giuseppe M Sangiorgi, MD sangiorgi.giuseppe@policlinico.mo.it Principal Investigator: Giuseppe Sangiorgi, MD Collapse <<

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.8719 mL
- 24.3593 mL
- 48.7187 mL
- 5 mM
- 0.9744 mL
- 4.8719 mL
- 9.7437 mL
- 10 mM
- 0.4872 mL
- 2.4359 mL
- 4.8719 mL

技术信息

CAS号

15421-84-8

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C10H15N5

运输

蓝冰

分子量

205.26

别名

AR-12008;Trapymin;Avantrin;Triazolopyrimidine;唑嘧胺

溶解度

DMSO	215.0 mg/mL (1047.5 mM)
Water	490.0 mg/mL (2387.2 mM)

动物实验配方

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