Trequinsin hydrochloride - CAS 78416-81-6
Category: Inhibitor
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Molecular Formula:
C24H27N3O3.HCl
Molecular Weight:
441.95
COA:
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Targets:
Phosphodiesterase (PDE)
Description:
Trequinsin hydrochloride is a highly potent inhibitor of cGMP-inhibited phosphodiesterase (PDE3) (IC50 = 250 pM). Trequinsin stimulates cAMP accumulation at a concentration of 10 µM, and inhibits arachidonic acid-induced platelet aggregation (IC50 = 50 pM). Trequinsin was shown to decrease blood pressure levels in both normotensive and hypertensive animal models and is used as an antihypertensive agent.
Brife Description:
PDE3 inhibitor
Purity:
≥97% by HPLC
Related CAS:
79855-88-2 (free base)
Synonyms:
2,3,6,7-Tetrahydro-9,10-dimethoxy-3-methyl-2-[(2,4,6-trimethylphenyl)imino]-4H-pyrimido[6,1-a]isoquinolin-4-one hydrochloride
MSDS:
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Application:
antihypertensive agent
InChIKey:
DTCZZBVPTHVXFA-UHFFFAOYSA-N
InChI:
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
Canonical SMILES:
CC1=CC(=C(C(=C1)C)N=C2C=C3C4=CC(=C(C=C4CCN3C(=O)N2C)OC)OC)C.Cl
1.YC-1 inhibited human platelet aggregation through NO-independent activation of soluble guanylate cyclase.
Wu CC;Ko FN;Kuo SC;Lee FY;Teng CM Br J Pharmacol. 1995 Oct;116(3):1973-8.
1. Our previous study demonstrated that YC-1, a derivative of benzylindazole, is a novel activator of soluble guanylate cyclase (sGC) in rabbit platelets. This work investigated whether the antiplatelet effect of YC-1 was mediated by a nitric oxide (NO)/sGC/cyclic GMP pathway in human platelets. 2. In human washed platelets, YC-1 inhibited platelet aggregation and ATP released induced by U46619 (2 microM), collagen (10 micro ml(-1)) and thrombin (0.1 u ml(-1)) in a concentration-dependent manner with IC50 values of (microM) 2.1 +/- 0.03, 11.7 +/- 2.1 and 59.3 +/- 7.1, respectively. 3. In a 30,000 g supernatant fraction from human platelet homogenate, YC-1 (5-100 microM) increased sGC activity in a concentration-dependent manner. At the same concentration-range, YC-1 elevated cyclic GMP levels markedly, but only slightly elevated cyclic AMP levels in the intact platelets. 4. MY-5445, a selective inhibitor of cyclic GMP phosphodiesterase, potentiated the increases in cyclic GMP caused by YC-1, and shifted the concentration-anti-aggregation curve of YC-1 to the left. In contrast, HL-725, a selective inhibitor of cyclic AMP phosphodiesterase, did not affect either the increases in cyclic nucleotides or the anti-aggregatory effect caused by YC-1.
2.Atrial natriuretic peptide reduces cyclic AMP by activating cyclic GMP-stimulated phosphodiesterase in vascular endothelial cells.
Kishi Y;Ashikaga T;Watanabe R;Numano F J Cardiovasc Pharmacol. 1994 Sep;24(3):351-7.
Bovine aortic endothelial cells contain cyclic GMP-stimulated phosphodiesterase (PDE) regulating intracellular cyclic AMP and cyclic GMP levels. To investigate the roles of this PDE isoform for cyclic AMP hydrolysis in intact endothelial cells (EC), we used an adenine prelabeling method to determine cyclic AMP accumulation in response to agents that might produce effects that increase cyclic GMP levels. Atrial natriuretic peptide (ANP), which dramatically increased cyclic GMP accumulation, reduced cyclic AMP in cultured EC from bovine aorta with or without addition of L-isoproterenol (L-ISO), whereas sodium nitroprusside (SNP) and 8-bromo cyclic GMP had no effect. The reduction in cyclic AMP by ANP was dose dependent (> or = 1.0 nM) and rapid (significant reduction was induced in < or = 15 s) and was abolished when EC were preincubated with 3-isobutyl-1-methylxanthine (IBMX) and HL-725, both nonselective PDE inhibitors. ANP had no effects on adenylate cyclase activity, nor any direct effects on the activities of partially purified cyclic GMP-stimulated PDE isoform or cyclic AMP-specific isoform. However, cyclic AMP hydrolyzing activities of EC were enhanced when EC were pretreated with 0.
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CAS 78416-81-6 Trequinsin hydrochloride

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