Trequinsin  (Synonyms: HL 725 free base)

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].

Trequinsin (40 μM; 82 min) induces a high-magnitude increase in intracellular calcium in pooled capacitated human donor sperm, equivalent to 91% of the response evoked by 10 μM Progesterone (HY-N0437)^[1].
Trequinsin (0.1-30 μM) induces a concentration-dependent increase in intracellular calcium in capacitated human donor sperm with an EC₅₀ of 3.43 μM, exhibits efficacy equivalent to progesterone at 10 μM, and cross-desensitises with PGE₁ but not progesterone^[1].
Trequinsin (10 μM; 120 min) significantly and sustainably increases hyperactivated motility in capacitated human donor sperm (80% density gradient centrifugation fraction) without altering total or progressive motility^[1].
Trequinsin (10 μM; 120 min) significantly increases progressive motility in poor-motility human donor sperm (40% density gradient centrifugation fraction) under both capacitating and non-capacitating conditions, and increases hyperactivated motility under capacitating conditions^[1].
Trequinsin (10 μM; 120 min) increases hyperactivated motility in the majority of capacitated human patient sperm samples, with no effect on total or progressive motility in most cases^[1].
Trequinsin (10 μM; 20 min) does not induce premature acrosome reaction in capacitated human donor sperm^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

405.50

C₂₄H₂₇N₃O₃

79855-88-2

O=C1N(C(=NC=2C(=CC(=CC2C)C)C)C=C3C=4C=C(OC)C(OC)=CC4CCN13)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.