79855-88-2
Chemical Structure
Trequinsin
Synonym(s): HL 725 free base
- CAS No.: 79855-88-2
- Formula:C24H27N3O3
- Molecular Weight:405.50
IUPAC Name: (E)-2-(mesitylimino)-9,10-dimethoxy-3-methyl-2,3,6,7-tetrahydro-4H-pyrimido[6,1-a]isoquinolin-4-one
InChIKey: MCMSJVMUSBZUCN-YYDJUVGSSA-N
SMILES: O=C1N(C(=NC=2C(=CC(=CC2C)C)C)C=C3C=4C=C(OC)C(OC)=CC4CCN13)C
Biological Activity: Trequinsin (HL 725 free base) is a PDE inhibitor, CatSper channel activator, and sperm potassium channel modulator. Trequinsin targets PDE3 with an IC50 of <1 nM. Trequinsin 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 significantly enhances sperm hyperactivated motility, forward motility, and the ability to penetrate viscous media. Trequinsin exerts age-specific positive inotropic and positive lusitropic effects on rabbit ventricular papillary muscles. Trequinsin has been used in studies on the mechanisms underlying male infertility (e.g., asthenozoospermia)[1][2].
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Trequinsin | Trequinsin (HL 725 free base) is a PDE inhibitor, CatSper channel activator, and sperm potassium channel modulator. Trequinsin targets PDE3 with an IC50 of <1 nM. Trequinsin 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 significantly enhances sperm hyperactivated motility, forward motility, and the ability to penetrate viscous media. Trequinsin exerts age-specific positive inotropic and positive lusitropic effects on rabbit ventricular papillary muscles. Trequinsin has been used in studies on the mechanisms underlying male infertility (e.g., asthenozoospermia). | |||||||||||||||||||||
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- [1]. McBrinn RC, et al. Novel pharmacological actions of trequinsin hydrochloride improve human sperm cell motility and function. Br J Pharmacol. 2019;176(23):4521-4536. [Content Brief]
- [2]. Oquist NL, et al. Inotropic responses to selective (RO 20-1724 and SQ 65,442) and nonselective (trequinsin) inhibitors of cyclic AMP-specific class IV phosphodiesterase in newborn, immature, and adult rabbit myocardium. Pediatr Res. 1992;31(3):300-304. [Content Brief]
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