Trequinsin hydrochloride (HL 725)

Cat No.:V72011 Purity: ≥98%
Trequinsin HCl (HL 725) is a potent inhibitor of platelet CAMP phosphodiesterase (PDE) with IC50 of 0.25 nM.
Trequinsin hydrochloride (HL 725) Chemical Structure CAS No.: 78416-81-6
Product category: Phosphodiesterase(PDE)
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
Trequinsin HCl (HL 725) is a potent inhibitor of platelet CAMP phosphodiesterase (PDE) with IC50 of 0.25 nM. Trequinsin HCl (HL 725) is a potent inhibitor of platelet aggregation induced by ADP, collagen, thrombin and epinephrine in vitro.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
In addition to its effects on the heart and blood pressure, trequinsin hydrochloride has strong antiplatelet properties[1]. Ca2+ iagonist trequinsin hydrochloride is effective[3].
Cell Assay
Cell Viability Assay[3]
Cell Types: Samples from healthy volunteer research donors with normal sperm motility parameters in agreement with World Health Organization 2010 criteria.
Tested Concentrations: 10 μM.
Incubation Duration: 20 min.
Experimental Results: Caused a concentrationdependent increase in [Ca2+]i (EC50 = 6.4 μM [95% confidence interval (CI): 4.1-9.9 μM]).
References
[1]. D Ruppert,, et al. HL 725, an extremely potent inhibitor of platelet phosphodiesterase and induced platelet aggregation in vitro. Life Sci. 1982 Nov 8;31(19):2037-43.
[2]. 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.
[3]. 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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H28CLN3O3
Molecular Weight
441.95
CAS #
78416-81-6
SMILES
CC1=CC(=C(C(=C1)C)/N=C/2\C=C3C4=CC(=C(C=C4CCN3C(=O)N2C)OC)OC)C.Cl
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 62.5 mg/mL (141.42 mM)
H2O: 50 mg/mL (113.13 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (4.71 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (4.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2627 mL 11.3135 mL 22.6270 mL
5 mM 0.4525 mL 2.2627 mL 4.5254 mL
10 mM 0.2263 mL 1.1313 mL 2.2627 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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