Trapidil (Rocornal, Trapymin, Avantrin, Trapymine) is an antagonist of PDGF, which can inhibit the proliferation of glioma cells producing PDGF.

 

Brand: BCM

 

Target: PDGFR; PDE

 

Signaling Pathways: Angiogenesis; Metabolism; Tyrosine Kinase/Adaptors

 

In Vitro: Trapidil interrupts the autocrine loop at the PDGF and PDGF-receptor level.Trapidil has proved to possess a significant antiproliferative activity. The addition of 100 to 400 μg/ml trapidil significantly reduced cell proliferation induced by different growth factors (FCS, PDGF-BB, bFGF, EGF), the highest inhibitory effect being on PDGF-BB stimulated Mesangial cell(MC) growth. The effect of the drug was dose-dependent and seemingly specific. Trapidil is an anti-platelet drug active against various aggregating agents, such as collagen, ADP, arachidonic acid, PAF and calcium ionophore. It exerts its action by blocking the biosynthesis of thromboxane A2 and antagonizing its effect at the receptor level, and by stimulating the synthesis and release of prostacyclin. Trapidil strongly inhibited osteoclast formation in co-cultures of bone marrow cells and osteoblasts without affecting receptor activator of NF-κB ligand (RANKL) or osteoprotegerin expression in osteoblasts. In addition, trapidil suppressed RANKL-induced osteoclast formation from osteoclast precursors. Trapidil reduced RANKL-induced expression of nuclear factor of activated T cells, cytoplasmic 1 (NFATc1), a master transcription factor for osteoclastogenesis, without affecting the expression of c-Fos that functions as a key upstream activator of NFATc1 during osteoclastogenesis. Trapidil has also been reported to inhibit phosphodiesterase, thromboxane A2, and CD40 signaling and activate protein kinase A.

 

In Vivo: Trapidil is an antiplatelet drug with specific platelet-derived growth factor antagonism and antiproliferative effects in the rat and rabbit models after balloon angioplasty. Trapidil had a potent inhibitory effect on osteoclast formation and bone resorption induced by interleukin-1 in an animal model. No abnormal symptoms, such as changes in body weight, diarrhea, high fever, and convulsion, were observed after intraperitoneal injections of trapidil.

 

Melting Point: 98-99.4° (Pfeifer); 102-104° from heptane (Tenor)

 

Solubility: Soluble in DMSO; Soluble in Water; Soluble in Ethanol.

 

GHS: GHS07

 

Isomeric SMILES: CCN(CC)C1=CC(=NC2=NC=NN12)C  

 

InChIKey: GSNOZLZNQMLSKJ-UHFFFAOYSA-N  

 

InChI: InChI=1S/C10H15N5/c1-4-14(5-2)9-6-8(3)13-10-11-7-12-15(9)10/h6-7H,4-5H2,1-3H3

 

Attribute
[Chem Name]	N,N-diethyl-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
[Synonym]	Trapidil; Rocornal; Trapymin; Avantrin; Trapymine
[CAS No.]	15421-84-8
[EINECS]	239-434-2
[MDL No.]	MFCD00193104
[Formula]	C10H15N5
[Molecular]	205.26
[Form]	White to tan powder
[Storage]	Inert atmosphere. Room Temperature

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