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Trapidil

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Chemical Structure| 15421-84-8 同义名 : 乐可安 ;AR-12008;Triazolopyrimidine;Trapymine;Avantrin;Trapymin;Rocornal
CAS号 : 15421-84-8
货号 : A569374
分子式 : C10H15N5
纯度 : 98%
分子量 : 205.26
MDL号 : MFCD00193104
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(511.55 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(487.19 mM)
动物实验配方：
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].
临床研究
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 ... 展开 >> Acute Coronary Syndrome 收起 << Phase 4 Unknown October 2012 Italy ... 展开 >> University Hospital Modena Recruiting Modena, Italy Contact: Giuseppe M Sangiorgi, MD       sangiorgi.giuseppe@policlinico.mo.it    Principal Investigator: Giuseppe Sangiorgi, MD 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.87mL

0.97mL

0.49mL

24.36mL

4.87mL

2.44mL

48.72mL

9.74mL

4.87mL
参考文献

[1]Kim SD, Kim HN, et al. Trapidil, a platelet-derived growth factor antagonist, inhibits osteoclastogenesis by down-regulating NFATc1 and suppresses bone loss in mice. Biochem Pharmacol. 2013 Sep 15;86(6):782-90.

[2]Maresta A, Balducelli M, et al. Trapidil (triazolopyrimidine), a platelet-derived growth factor antagonist, reduces restenosis after percutaneous transluminal coronary angioplasty. Results of the randomized, double-blind STARC study. Studio Trapidil versus Aspirin nella Restenosi Coronarica. Circulation. 1994 Dec;90(6):2710-5.

[3]Kuratsu J, Ushio Y. Antiproliferative effect of trapidil, a platelet-derived growth factor antagonist, on a glioma cell line in vitro. J Neurosurg. 1990 Sep;73(3):436-40. doi: 10.3171/jns.1990.73.3.0436. PMID: 2384782.

[4]Kim SD, Kim HN, Lee JH, Jin WJ, Hwang SJ, Kim HH, Ha H, Lee ZH. Trapidil, a platelet-derived growth factor antagonist, inhibits osteoclastogenesis by down-regulating NFATc1 and suppresses bone loss in mice. Biochem Pharmacol. 2013 Sep 15;86(6):782-90. doi: 10.1016/j.bcp.2013.07.015. Epub 2013 Aug 6. PMID: 23928189.

[5]Gesualdo L, Di Paolo S, Ranieri E, Schena FP. Trapidil inhibits human mesangial cell proliferation: effect on PDGF beta-receptor binding and expression. Kidney Int. 1994 Oct;46(4):1002-9. doi: 10.1038/ki.1994.360. PMID: 7861694.

[6]Hoshiya M, Awazu M. Trapidil inhibits platelet-derived growth factor-stimulated mitogen-activated protein kinase cascade. Hypertension. 1998 Feb;31(2):665-71. doi: 10.1161/01.hyp.31.2.665. PMID: 9461238.