Trequinsin hydrochloride
Based on 1 Customer Validation
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).
For research use only. We do not sell to patients.
- Purity: 99.86%
- CAS No.: 78416-81-6
- Formula: C24H28ClN3O3
- Molecular Weight:441.95
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Bioactive Compound Library Max
HY-L181
-
Bioactive Compound Library
HY-L001
-
Metabolism/Protease Compound Library
HY-L012
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Alzheimer's Disease Compound Library
HY-L069
-
Neurodegenerative Disease-related Compound Library
HY-L086
-
Anti-Colorectal Cancer Compound Library
HY-L103
-
Metabolic Enzyme Compound Library
HY-L146
-
Highly Selective Inhibitors Library
HY-L158
-
MCE Bioactive Compound Library
HY-L001V
-
High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
|
PDE3 |
Trequinsin hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride (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.
-
Cell Line:Samples from healthy volunteer research donors with normal sperm motility parameters in agreement with World Health Organization 2010 criteria.
-
Concentration:10 μM.
-
Incubation Time:20 min.
-
Result:Caused a concentrationdependent increase in [Ca2+]i (EC50 = 6.4 μM [95% confidence interval (CI): 4.1-9.9 μM]).
Chemical Information
-
CAS No. 78416-81-6
-
Appearance Solid
-
Molecular Weight 441.95
-
Formula C24H28ClN3O3
-
Color Light yellow to yellow
-
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
-
Synonyms
HL 725
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 62.5 mg/mL (141.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (113.13 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
-
Data Sheet (278 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.2627 mL | 11.3135 mL | 22.6270 mL | 56.5675 mL |
| 5 mM | 0.4525 mL | 2.2627 mL | 4.5254 mL | 11.3135 mL | |
| 10 mM | 0.2263 mL | 1.1313 mL | 2.2627 mL | 5.6567 mL | |
| 15 mM | 0.1508 mL | 0.7542 mL | 1.5085 mL | 3.7712 mL | |
| 20 mM | 0.1131 mL | 0.5657 mL | 1.1313 mL | 2.8284 mL | |
| 25 mM | 0.0905 mL | 0.4525 mL | 0.9051 mL | 2.2627 mL | |
| 30 mM | 0.0754 mL | 0.3771 mL | 0.7542 mL | 1.8856 mL | |
| 40 mM | 0.0566 mL | 0.2828 mL | 0.5657 mL | 1.4142 mL | |
| 50 mM | 0.0453 mL | 0.2263 mL | 0.4525 mL | 1.1313 mL | |
| 60 mM | 0.0377 mL | 0.1886 mL | 0.3771 mL | 0.9428 mL | |
| 80 mM | 0.0283 mL | 0.1414 mL | 0.2828 mL | 0.7071 mL | |
| 100 mM | 0.0226 mL | 0.1131 mL | 0.2263 mL | 0.5657 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Trequinsin hydrochloride Related Classifications
HY-18740A Related Classifications
Powered by Bioz