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Biological Activity for Trequinsin hydrochloride
Trequinsin hydrochloride is a 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 for Trequinsin hydrochloride
Technical Data for Trequinsin hydrochloride
|Storage||Desiccate at RT|
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 for Trequinsin hydrochloride
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Trequinsin hydrochloride
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.
|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|
Product Datasheets for Trequinsin hydrochloride
References for Trequinsin hydrochloride
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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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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