78416-81-6
Chemical Structure
Trequinsin hydrochloride
Synonym(s): HL 725
- CAS No.: 78416-81-6
- Formula:C24H28ClN3O3
- Molecular Weight:441.95
IUPAC Name: (E)-2-(mesitylimino)-9,10-dimethoxy-3-methyl-2,3,6,7-tetrahydro-4H-pyrimido[6,1-a]isoquinolin-4-one hydrochloride
InChIKey: DTCZZBVPTHVXFA-OSMRDGEFSA-N
SMILES: O=C(N(CCC1=C2C=C(OC)C(OC)=C1)C2=C/3)N(C)C3=N\C4=C(C)C=C(C)C=C4C.[H]Cl
Biological Activity: Trequinsin hydrochloride (HL 725) is a PDE inhibitor, CatSper channel activator, and sperm potassium channel modulator. Trequinsin hydrochloride targets PDE3 with an IC50 of <1 nM. Trequinsin hydrochloride enhances currents and elevates intracellular calcium and cGMP levels via direct activation of the CatSper channel, while inhibiting the outward current conductance of sperm potassium channels. Without inducing premature acrosome reaction, Trequinsin hydrochloride significantly enhances sperm hyperactivated motility, forward motility, and the ability to penetrate viscous media. Trequinsin hydrochloride exerts age-specific positive inotropic and positive lusitropic effects on rabbit ventricular papillary muscles. Trequinsin hydrochloride has been used in studies on the mechanisms underlying male infertility (e.g., asthenozoospermia)[1][2].
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Trequinsin hydrochloride | 99.86% | Trequinsin hydrochloride (HL 725) is a PDE inhibitor, CatSper channel activator, and sperm potassium channel modulator. Trequinsin hydrochloride targets PDE3 with an IC50 of <1 nM. Trequinsin hydrochloride enhances currents and elevates intracellular calcium and cGMP levels via direct activation of the CatSper channel, while inhibiting the outward current conductance of sperm potassium channels. Without inducing premature acrosome reaction, Trequinsin hydrochloride significantly enhances sperm hyperactivated motility, forward motility, and the ability to penetrate viscous media. Trequinsin hydrochloride exerts age-specific positive inotropic and positive lusitropic effects on rabbit ventricular papillary muscles. Trequinsin hydrochloride has been used in studies on the mechanisms underlying male infertility (e.g., asthenozoospermia). | ||||||||||||||||||||
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- [1]. K C Agarwal, et al. Role of plasma adenosine in the antiplatelet action of HL 725, a potent inhibitor of cAMP phosphodiesterase: species differences. Thromb Res. 1987 Jul 15;47(2):191-200. [Content Brief]
- [2]. Rachel C McBrinn, et al. Novel pharmacological actions of trequinsin hydrochloride improve human sperm cell motility and function. Br J Pharmacol. 2019 Dec;176(23):4521-4536. [Content Brief]
Keywords
