T2057
Trequinsin hydrochloride
≥98%
别名:
HL 725
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关于此项目
经验公式（希尔记法）:
C24H27N3O3 · HCl
化学文摘社编号:
分子量:
441.95
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
41106305
MDL number:
InChI
1S/C24H27N3O3.ClH/c1-14-9-15(2)23(16(3)10-14)25-22-13-19-18-12-21(30-6)20(29-5)11-17(18)7-8-27(19)24(28)26(22)4;/h9-13H,7-8H2,1-6H3;1H/b25-22+;
SMILES string
Cl[H].COc1cc2CCN3C(=O)N(C)C(\C=C3c2cc1OC)=N\c4c(C)cc(C)cc4C
InChI key
DTCZZBVPTHVXFA-OSMRDGEFSA-N
assay
≥98%
form
powder
Quality Level
Gene Information
human ... PDE3A(5139), PDE3B(5140)
Application
Trequinsin has been used as a PDE3 inhibitor in rat juxtaglomerular cells. This study reported that trequinsin can enhance cellular cAMP content, forskolin-induced cAMP synthesis, and renin release in cells.
Biochem/physiol Actions
Phosphodiesterase III inhibitor.
Trequinsin is a strong antihypertensive agent that has a hemodynamic profile similar to that of arteriolar dilators. Trequinsin can block platelet aggregation and also inhibit tissue factor expression in human endothelial cells,.
Features and Benefits
This compound is a featured product for Cyclic Nucleotide research. Click here to discover more featured Cyclic Nucleotide products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the Phosphodiesterases page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
R F Booth et al.
Biochemical pharmacology, 36(20), 3517-3521 (1987-10-15)
The discovery and structure-activity of a new class of renal artery phosphodiesterase inhibitors is reported, some of which are highly selective for the guanosine cyclic 3',5'-monophosphate phosphodiesterase. One of these compounds, 5,6-dihydro-8,9,11,12-tetramethoxy-1,3-dioxo-1H-benz[f]- isoquino [8,1,2- hij]quinazoline-2(3H)-carboxylic acid, ethyl ester (9), is
R A Rius et al.
Life sciences, 54(22), 1735-1743 (1994-01-01)
In primary cultured bovine adrenal chromaffin cells (BACC), pituitary adenylate cyclase activating polypeptide 1-38 (PACAP) produced a dose related increase in tyrosine hydroxylase (TH) Vmax when measured 48 hours after the beginning of the treatment; a significant increase was observed
R Pillai et al.
The Journal of biological chemistry, 269(48), 30676-30681 (1994-12-02)
We have created a series of deletion mutants of a human cardiac cAMP phosphodiesterase in order to define sequences necessary for function and to identify residues required for inhibition by cGMP and by the drugs milrinone and trequinsin. These truncated
Jorge E Torres-López et al.
European journal of pharmacology, 519(1-2), 75-79 (2005-08-23)
The local peripheral (subcutaneous) injection of phosphodiesterase 3 inhibitor trequinsin dose-dependently enhanced formalin-evoked flinching during late second phase of this test. Treatment with the nitric oxide synthase inhibitor N-L-nitro-arginine methyl ester or guanylyl cyclase inhibitor 1-H-[1,2,4,]oxadiazolo[4,3-a]quinoxalin-1-one significantly reversed trequinsin-induced pronociceptive
N E Leclerc et al.
Journal of cardiovascular pharmacology, 25 Suppl 2, S88-S91 (1995-01-01)
Exposure of endothelial cells (ECs) to thrombin or cytokines leads to major changes in their biochemical properties, which confer procoagulant activities. Stimulated ECs express the procoagulant glycoprotein tissue factor (TF). Although some TF is expressed on the apical surface of
商品
Cyclic nucleotides like cAMP modulate cell function via PKA activation and ion channels.
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