Biological Activity
Extremely potent inhibitor of cGMP-inhibited phosphodiesterase (PDE3; IC50 = 250 pM). Potently inhibits arachidonic acid-induced aggregation of human platelets (IC50 = 50 pM). Orally active antihypertensive agent; reduces systemic blood pressure in both normotensive and hypertensive animal models.
Compound Libraries
Trequinsin hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 441.95 |
| Formula | C24H27N3O3.HCl |
| Storage | Desiccate at RT |
| Purity | ≥97% (HPLC) |
| CAS Number | 78416-81-6 |
| PubChem ID | 3060974 |
| InChI Key | DTCZZBVPTHVXFA-UHFFFAOYSA-N |
| Smiles | Cl.COC1=C(OC)C=C2C(CCN3C(=O)N(C)C(C=C23)=NC2=C(C)C=C(C)C=C2C)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 44.2 | 100 | |
| ethanol | 44.2 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 441.95. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.26 mL | 11.31 mL | 22.63 mL |
| 5 mM | 0.45 mL | 2.26 mL | 4.53 mL |
| 10 mM | 0.23 mL | 1.13 mL | 2.26 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Ruppert and Weithmann (1982) HL 725, an extremely potent inhibitor of platelet phosphodiesterase and induced platelet aggregation in vitro. Life Sci. 31 2037 PMID: 6294426
Lal et al (1984) Trequinsin, a potent new antihypertensive vasodilator in the series of 2-(arylimino)-3-alkyl-9,10-dimethoxy-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-ones. J.Med.Chem. 27 1470 PMID: 6492077
Agarwal et al (1987) Role of plasma adenosine in the antiplatelet action of HL 725, a potent inhibitor of cAMP phosphodiesterase: species differences. Thromb.Res. 47 191 PMID: 2821650
Keywords: Trequinsin hydrochloride, supplier, Ultrapotent, inhibitors, inhibits, PDE3, Phosphodiesterases, HL725, HL-725, Phosphodiesterases, Phosphodiesterases, Tocris Bioscience
