A cAMP-dependent PDE3 inhibitor (IC50s = 0.04 and 0.03 nM for PDE3A and PDE3B

Trequinsin (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
78416-81-6
Storage:
-20
UN-No:
Non-Hazardous - /

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.{39526} 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.{39523} 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.{39524} 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.{39522}  

 

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Description

A cAMP-dependent PDE3 inhibitor (IC50s = 0.04 and 0.03 nM for PDE3A and PDE3B, respectively in T84 cell lysates); stimulates cAMP accumulation (10 µM) and increases membrane capacitance in rat juxtaglomerular cells; competitively inhibits multidrug resistant protein 5-mediated export of cGMP from Chinese hamster lung fibroblasts (Ki = 240 nM); reduces collagen-induced platelet aggregation in rabbits (3 µg/kg per minute); reduces collagen-induced decreases in mean arterial blood pressure alone or in combination with prostacyclin

Formal name: 2,3,6,7-tetrahydro-9,10-dimethoxy-3-methyl-2-[(2,4,6-trimethylphenyl)imino]-4H-pyrimido[6,1-a]isoquinolin-4-one, monohydrochloride

Synonyms: 

Molecular weight: 442

CAS: 78416-81-6

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phosphodiesterases||Research Area|Cardiovascular System|Blood|Thrombosis

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