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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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T413174-5mg | 5mg | In stock | $49.90 | |
T413174-10mg | 10mg | In stock | $82.90 | |
T413174-25mg | 25mg | In stock | $186.90 | |
T413174-50mg | 50mg | In stock | $284.90 |
PDGFR Antagonists
Synonyms | trapidil | 15421-84-8 | Rocornal | Trapymin | Avantrin | Trapymine | N,N-diethyl-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | AR 12008 | AR-12008 | (1,2,4)Triazolo(1,5-a)pyrimidin-7-amine, N,N-diethyl-5-methyl- | 7-Diethylamino-5-methyl-s-triazolo(1,5-a)pyrimidine | MLS0 |
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Specifications & Purity | ≥98% |
Biochemical and Physiological Mechanisms | Trapidil (Rocornal, Trapymin, Avantrin, Trapymine) is a PDGF antagonist that can inhibit the proliferation of the PDGF-producing glioma cells. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | Information Trapidil Trapidil (Rocornal, Trapymin, Avantrin, Trapymine) is a PDGF antagonist that can inhibit the proliferation of the PDGF-producing glioma cells. Targets PDGF 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. Cell Research(from reference) Cell lines:Human Mesangial cell lines Concentrations:100 μg/ml Incubation Time:96 h |
ALogP | 1.922 |
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Rotatable Bond | 3 |
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IUPAC Name | N,N-diethyl-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine |
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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 |
InChi Key | GSNOZLZNQMLSKJ-UHFFFAOYSA-N |
Canonical SMILES | CCN(CC)C1=CC(=NC2=NC=NN12)C |
Isomeric SMILES | CCN(CC)C1=CC(=NC2=NC=NN12)C |
PubChem CID | 5531 |
Molecular Weight | 205.26 |
Enter Lot Number to search for COA:
To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section
Lot Number | Certificate Type | Date | Item |
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C2304097 | Certificate of Analysis | Oct 20, 2022 | T413174 |
C2304101 | Certificate of Analysis | Oct 20, 2022 | T413174 |
C2304102 | Certificate of Analysis | Oct 20, 2022 | T413174 |
C2304103 | Certificate of Analysis | Oct 20, 2022 | T413174 |
Solubility | Solubility (25°C) In vitro DMSO: 41 mg/mL (199.74 mM); Water: 41 mg/mL (199.74 mM); Ethanol: 41 mg/mL (199.74 mM); |
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DMSO(mg / mL) Max Solubility | 41 |
DMSO(mM) Max Solubility | 199.7466628 |
Water(mg / mL) Max Solubility | 41 |
Water(mM) Max Solubility | 199.7466628 |
Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation |
Precautionary Statements | P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of water. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P271:Use only outdoors or in a well-ventilated area. P304+P340:IF INHALED: Remove person to fresh air and keep comfortable for breathing. P403+P233:Store in a well-ventilated place. Keep container tightly closed. P362+P364:Take off contaminated clothing and wash it before reuse. P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes. P337+P317:If eye irritation persists: Get medical help. P332+P317:If skin irritation occurs: Get medical help. P319:Get medical help if you feel unwell. |