Trequinsin hydrochloride

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Cat.No. 2337 - Trequinsin hydrochloride | C24H27N3O3.HCl | CAS No. 78416-81-6
Description: Highly potent PDE3 inhibitor
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 (1)
Reviews
Literature (2)

Biological Activity

Highly 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. Also activates CatSper channels, increases intracellular Ca2+ and cGMP levels, and decreases potassium channel activity in sperm.

Compound Libraries

Trequinsin hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 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)=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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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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References

References are publications that support the biological activity of the product.

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

McBrinn et al (2019) Novel pharmacological actions of Trequinsin Hydrochloride improve human sperm cell motility and function. Br.J.Pharmacol. PMID: 31368510


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View all Phosphodiesterase Inhibitors

Keywords: Trequinsin hydrochloride, Trequinsin hydrochloride supplier, Ultrapotent, inhibitors, inhibits, PDE3, Phosphodiesterases, HL725, Catsper, activators, activates, sperm, motility, HL-725, Other, Calcium, Channels, 2337, Tocris Bioscience

1 Citation for Trequinsin hydrochloride

Citations are publications that use Tocris products. Selected citations for Trequinsin hydrochloride include:

McBrinn et al (2019) Novel pharmacological actions of Trequinsin Hydrochloride improve human sperm cell motility and function. Br.J.Pharmacol. 176 4521 PMID: 31368510


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