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100mg |
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500mg |
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1g |
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Dipyridamole (also known as NSC515776; RA8; Persantine) is a pyrimido-pyrimidine based phosphodiesterase (PDE) inhibitor with antiplatelet properties. It blocks the uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole is used in combination with 'blood thinners' such as warfarin to prevent the formation of blood clots after heart valve replacement surgery.
ln Vitro |
In OCI-AML-3 cells, dipyridamole (5 μM; 15 min) increased intracellular cAMP levels 2.5-fold [2]. Primary AML cells undergo apoptosis when statins and dipyridamole (5 μM; 48 hours) are combined [2]. Dipyridamole (5 μM; 48 hours) inhibits statin-induced SREBP2 activation in a cAMP/PKA-independent manner [2].
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ln Vivo |
Dipyridamole (10 mg/kg); taken orally, once daily for eighteen days) inhibits the growth of tumors, enhances blood flow while simultaneously altering the tumor's tissue, and increases platelet infiltration [3].
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Cell Assay |
Apoptosis Analysis[2]
Cell Types: AML (OCI-AML-2, OCI-AML-3) cell line Tested Concentrations: 5 μM Incubation Duration: 48 h Experimental Results: Induced apoptosis with the combination of fluvastatin and dipyridamole, cilostazol, forskolin, or dbcAMP in OCI-AML-2 and OCI-AML-3 cells. RT-PCR[2] Cell Types: LP1 cell line Tested Concentrations: 5 μM Incubation Duration: 16 h Experimental Results: Increased the sensibility of cancer cells to statin-induced apoptosis. |
Animal Protocol |
Animal/Disease Models: C57BL/6-LLC tumor-bearing mouse model [3]
Doses: 10 mg/kg Route of Administration: po (oral gavage); 10 mg/kg; one time/day for 18 days Experimental Results: Reduce tumors in tumor-bearing mice grow. |
References |
[1]. Kerndt CC, Nagalli S. Dipyridamole. 2021 Nov 25. In: StatPearls . Treasure Island (FL): StatPearls Publishing; 2022 Jan–. PMID: 32119342.
[2]. Longo, Joseph, etal. Cyclic AMP-hydrolyzing phosphodiesterase inhibitors potentiate statin-induced cancer cell death. Molecular oncology vol. 14,10 (2020): 2533-2545 [3]. Wang, Jiaan-Der, etal. Exosomal HMGB1 Promoted Cancer Malignancy. Cancers vol. 13,4 877. 19 Feb. 2021. |
Molecular Formula |
C24H40N8O4
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Molecular Weight |
504.63
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CAS # |
58-32-2
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Related CAS # |
Dipyridamole-d20;1189983-52-5;Dipyridamole-d16
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SMILES |
OCCN(CCO)C1=NC(N2CCCCC2)=C(N=C(N(CCO)CCO)N=C3N4CCCCC4)C3=N1
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InChi Key |
IZEKFCXSFNUWAM-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C24H40N8O4/c33-15-11-31(12-16-34)23-26-20-19(21(27-23)29-7-3-1-4-8-29)25-24(32(13-17-35)14-18-36)28-22(20)30-9-5-2-6-10-30/h33-36H,1-18H2
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Chemical Name |
2,2,2,2-((4,8-di(piperidin-1-yl)pyrimido[5,4-d]pyrimidine-2,6-diyl)bis(azanetriyl))tetraethanol
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.95 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.95 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9816 mL | 9.9082 mL | 19.8165 mL | |
5 mM | 0.3963 mL | 1.9816 mL | 3.9633 mL | |
10 mM | 0.1982 mL | 0.9908 mL | 1.9816 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT02121756 | Completed Has Results | Drug: Dipyridamole Drug: Placebo, then Dipyridamole |
HIV Infection | Sharon Riddler | July 2014 | Phase 1 Phase 2 |
NCT04424901 | Terminated Has Results | Drug: Placebo Drug: Dipyridamole Tablets |
COVID-19 Pneumonia Vascular Complications |
UConn Health | May 3, 2020 | Phase 2 |
NCT01613755 | Completed | Drug: Metformin, dipyridamole Drug: Metformin |
Diabetes | Radboud University Medical Center | April 2012 | Phase 4 |
NCT00457405 | Completed | Ischemia-Reperfusion Injury | Radboud University Medical Center | June 2007 | Phase 4 |
Dipyridamole inhibits the sterol‐regulated feedback loop of the MVA pathway. Schematic representation of the MVA pathway. Statins inhibit the rate‐limiting enzyme of the pathway, HMGCR, which catalyzes the conversion of HMG‐CoA to MVA. MVA is subsequently used to synthesize various metabolites that are important for cell growth and survival, including GGPP and cholesterol. Statin‐mediated cholesterol depletion induces the cleavage and activation of SREBP2, which in turn induces the transcription of genes involved in MVA metabolism to restore homeostasis. We previously identified that the drug dipyridamole can inhibit statin‐induced SREBP2 activation; however, the mechanism by which dipyridamole inhibits SREBP2 cleavage remains poorly understood. td> |
Dipyridamole mitigated LLC cell proliferation. td> |
Dipyridamole and GW4869 mitigated tumor growth. LLC cells or saline vehicle were implanted into C57BL/6 mice and allowed to grow for 3 weeks. Three days after implantation, dipyridamole (10 mg/kg) and GW4869 (2.5 mg/kg) were administrated daily up until the end of the experiment. The tumor volume (A), resected tumor tissues (B), and tumor mass (C) are shown. The total white blood cells (WBC) (D), sP-selectin (E), TGF-β1 (F), and platelets (G) in blood samples were determined. * p < 0.05 vs. saline or sham untreated group and # p < 0.05 vs. LLC untreated group, n = 8. td> |