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T2057

Sigma-Aldrich

Trequinsin hydrochloride

≥98%

Sinônimo(s):

HL 725

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About This Item

Fórmula empírica (Notação de Hill):
C24H27N3O3 · HCl
Número CAS:
78416-81-6
Peso molecular:
441.95
Número MDL:
MFCD01076563
Código UNSPSC:
41106305
ID de substância PubChem:
24278727
NACRES:
NA.77

Ensaio

≥98%

forma

powder

cadeia de caracteres SMILES

Cl[H].COc1cc2CCN3C(=O)N(C)C(\C=C3c2cc1OC)=N\c4c(C)cc(C)cc4C

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+;

chave InChI

DTCZZBVPTHVXFA-OSMRDGEFSA-N

Informações sobre genes

human ... PDE3A(5139) , PDE3B(5140)

Aplicação

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.

Ações bioquímicas/fisiológicas

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,.
Phosphodiesterase III inhibitor.

Características e benefícios

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.

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable

Equipamento de proteção individual

Eyeshields, Gloves, type N95 (US)

Certificados de análise (COA)

Busque Certificados de análise (COA) digitando o Número do Lote do produto. Os números de lote e remessa podem ser encontrados no rótulo de um produto após a palavra “Lot” ou “Batch”.

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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
J E Souness et al.
The Biochemical journal, 266(1), 127-132 (1990-02-15)
Two cyclic nucleotide phosphodiesterase (PDE) activities were identified in pig aortic endothelial cells, a cyclic GMP-stimulated PDE and a cyclic AMP PDE. Cyclic GMP-stimulated PDE had Km values of 367 microM for cyclic AMP and 24 microM for cyclic GMP
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
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
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
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Discover Bioactive Small Molecules for Cyclic Nucleotides

Cyclic nucleotides, including cyclic AMP (cAMP), cyclic GMP (cGMP) and cyclic ADP-ribose, have been extensively studied as second messengers of intracellular events initiated by activation of GPCRs. cAMP modifies cell function in all eukaryotic cells, principally through the activation of cAMP-dependent protein kinase (PKA), but also through cAMP-gated ion channels and guanine nucleotide exchange factors directly activated by cAMP.

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