trapidil
trapidil
CAS: 15421-84-8
Molecular Formula: C10H15N5
trapidil - Names and Identifiers
| Name | trapidil |
| Synonyms | Trapymin Avantrin TRAPIDIL trapidil 15421-84-8 7-(Diethylamino)-5-Methyl-S-Triazolo[1,5-A]Pyrimidine 7-(DIETHYLAMINO)-5-METHYL-S-TRIAZOLO[1,5-A]PYRIMIDINE 7-Diethylamino-5-methyl[1,2,4]triazolo[1,5-a]pyrimidine N,N-Diethyl-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine N,N-Diethyl-5-methyl-[1,2,4]triazolo[5,1-b]pyrimidin-7-amine N,N-Diethyl-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine [1,2,4]triazolo[1,5-a]pyrimidin-7-amine, N,N-diethyl-5-methyl- |
| CAS | 15421-84-8 |
| EINECS | 239-434-2 |
| InChI | InChI=1/C10H15N5/c1-4-14(5-2)9-6-8(3)13-10-11-7-12-15(9)10/h6-7H,4-5H2,1-3H3 |
trapidil - Physico-chemical Properties
| Molecular Formula | C10H15N5 |
| Molar Mass | 205.26 |
| Density | 1.20±0.1 g/cm3(Predicted) |
| Melting Point | 98-99.4° (Pfeifer); 102-104° from heptane (Tenor) |
| Solubility | H2O: ≥15mg/mL |
| Appearance | powder |
| Color | white to tan |
| pKa | pKs = 2.79(at 25℃) |
| Storage Condition | Inert atmosphere,Room Temperature |
| Refractive Index | 1.625 |
| Use | Used as an antianginal agent |
| In vitro study | Trapidil destroys the autocrine loop of PDGF and PDGF receptors and has significant antiproliferative activity. 100-400 μg/ml trapidil significantly reduced cell proliferation by different growth factors (FCS, PDGF-BB, bFGF, EGF), with inhibition of PDGF-BB being greatest. The effect of Trapidil is concentration-dependent and very specific. Trapidil is an anti-platelet aggregation drug with activity against a variety of inducers, such as collagen, ADP, arachidonic acid, PAF, and calcium ionophore. It acts by blocking the biosynthesis of thromboxane A2 and antagonizing it at the receptor level. Simultaneously Stimulates the biosynthesis and release of prostacyclin. Trapidil strongly inhibits osteoclast formation in the medium in which bone marrow cells and osteoblasts are co-cultured, without affecting the receptor activator of NF-κB ligand (RANKL) or the expression of Osteoprotegerin in osteoblasts. In addition, trapidil can also inhibit the differentiation of osteoclast precursors into osteoclasts induced by RANKL. Trapidil reduced RANKL-induced expression of the nuclear factor NFATc1 in activated T cells without affecting c-Fos expression. Trapidil has also been reported to inhibit phosphodiesterase, thromboxane A2, CD40 signaling pathway, and activated PKA. |
| In vivo study | Trapidil is an antiplatelet agent with specific antagonism to PDGF and antiproliferative effects after balloon angioplasty in rats and rabbits. In animal models, Trapidil has potent inhibitory effects on osteoclast formation and interleukin-1 induced bone resorption. After intraperitoneal injection of trapidil, there were no abnormal symptoms, such as weight change, Diarrhea, high fever, tremor and so on. |
trapidil - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| WGK Germany | 3 |
| Toxicity | LD50 in mice, rats (mg/kg): 115, 76 i.v.; 380, 235 orally; 155, 100 i.p.; 132, 100 s.c. (Fuller) |
trapidil - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 4.872 ml | 24.359 ml | 48.719 ml |
| 5 mM | 0.974 ml | 4.872 ml | 9.744 ml |
| 10 mM | 0.487 ml | 2.436 ml | 4.872 ml |
| 5 mM | 0.097 ml | 0.487 ml | 0.974 ml |
Last Update：2024-01-02 23:10:35
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