Trequinsin hydrochloride

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Cat.No. 2337 - Trequinsin hydrochloride | C24H27N3O3.HCl | CAS No. 78416-81-6
Description: Extremely potent inhibitor of PDE3
Alternative Names: HL-725
Chemical Name: 2,3,6,7-Tetrahydro-9,10-dimethoxy-3-methyl-2-[(2,4,6-trimethylphenyl)imino]-4H-pyrimido[6,1-a]isoquinolin-4-one hydrochloride
Purity: ≥97% (HPLC)
Datasheet
Citations
Literature

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

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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)=N\C2=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

Safety Datasheet

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


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Keywords: Trequinsin hydrochloride, supplier, Ultrapotent, inhibitors, inhibits, PDE3, Phosphodiesterases, HL725, HL-725, Phosphodiesterases, Phosphodiesterases, Tocris Bioscience

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