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Trequinsin hydrochloride

Catalog No.GC13495

PDE3 inhibitor

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Trequinsin hydrochloride Chemical Structure

Cas No.: 78416-81-6

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1mg
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5mg
$153.00
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10mg
$255.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

Trequinsin is a phosphodiesterase (PDE) 3 inhibitor that is dependent on cyclic AMP (cAMP), with IC50 values of 0.04 and 0.03 nM for PDE3A and PDE3B, respectively, in T84 human colonic adenocarcinoma cell lysates.[1] In cultured primary rat juxtaglomerular cells, trequinsin stimulates cAMP accumulation when used at a concentration of 10 µM and increases cell membrane capacitance in a patch clamp assay.[2] Trequinsin also competitively inhibits the multidrug resistant protein 5-mediated export of cGMP from Chinese hamster lung fibroblasts with a Ki value of 240 nM.[3] In vivo, trequinsin reduces collagen-induced platelet aggregation in rabbits when administered intravenously at a rate of 3 µg/kg per minute, as well as the collagen-induced decrease in mean arterial blood pressure when administered alone or in combination with prostacyclin.[4]

Reference:
[1]. Liu, S., Veilleux, A., Zhang, L., et al. Dynamic activation of cystic fibrosis transmembrane conductance regulator by type 3 and type 4D phosphodiesterase inhibitors. J. Pharmacol. Exp. Ther. 314(2), 846-854 (2005).
[2]. Friis, U.G., Jensen, B.L., Sethi, S., et al. Control of renin secretion from rat juxtaglomerular cells by cAMP-specific phosphodiesterases. Circ. Res. 90(9), 996-1003 (2002).
[3]. Jedlitschky, G., Burchell, B., and Keppler, D. The multidrug resistance protein 5 functions as an ATP-dependent export pump for cyclic nucleotides. J. Biol. Chem. 275(39), 30069-30074 (2000).
[4]. Darius, H., Lefer, A.M., Leprán, I., et al. In vivo interaction of prostacyclin with an inhibitor of cyclic nucleotide phosphodiesterase, HL 725. Br. J. Pharmacol. 84(3), 735-741 (1985).

Chemical Properties

Cas No. 78416-81-6 SDF
Chemical Name (E)-2-(mesitylimino)-9,10-dimethoxy-3-methyl-6,7-dihydro-2H-pyrimido[6,1-a]isoquinolin-4(3H)-one hydrochloride
Canonical SMILES O=C(N(C)/C1=N/C2=C(C)C=C(C)C=C2C)N(C(C3=C4)=C1)CCC3=CC(OC)=C4OC.Cl
Formula C24H27N3O3.HCl M.Wt 441.95
Solubility 100mM in ethanol, or in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.2627 mL 11.3135 mL 22.627 mL
5 mM 0.4525 mL 2.2627 mL 4.5254 mL
10 mM 0.2263 mL 1.1313 mL 2.2627 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 11 reference(s) in Google Scholar.)

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