Name: Trapidil
Brand: Selleck Chemicals
SKU: S4736
Availability: InStock
Rating: 5 (8 reviews)

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Quality Control

Batch: Purity: 99.94%

99.94

Related Targets	EGFR VEGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit
Other PDGFR Inhibitors	CP-673451 Crenolanib Orantinib (SU6668) Tyrphostin AG 1296 PP121 AZD2932 Sennoside B Tyrphostin AG1433 AG 1295 N-(p-Coumaroyl) Serotonin

Solubility

In vitro
Batch:

DMSO : 41 mg/mL (199.74 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 41 mg/mL

Ethanol : 41 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	205.26	Formula	C₁₀H₁₅N₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	15421-84-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Rocornal, Trapymin, Avantrin, Trapymine			Smiles	CCN(CC)C1=CC(=NC2=NC=NN12)C

Mechanism of Action

Targets/IC₅₀/Ki	PDGF
In vitro	Trapidil interrupts the autocrine loop at the PDGF and PDGF-receptor level. This compound has proved to possess a significant antiproliferative activity. The addition of 100 to 400 μg/ml of this chemical 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. It 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. This agent 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, it suppressed RANKL-induced osteoclast formation from osteoclast precursors. The compound 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. It 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. This compound 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 this chemical.
References	[1] https://pubmed.ncbi.nlm.nih.gov/7994812/ [2] https://pubmed.ncbi.nlm.nih.gov/7861694/ [3] https://pubmed.ncbi.nlm.nih.gov/23928189/

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Trapidil PDGFR antagonist

Chemical Structure

Molecular Weight: 205.26