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T7692

T-1032

Name: T-1032
Brand: SIGMA

>99% (HPLC), solid

Synonym(s):

Methyl (2-(4-aminophenyl)-1,2-dihydro-1-oxo-7-(2-pyridinylmethoxy)-4-(3,4,5-trimethoxyphenyl)-3-isoquinoline carboxylate sulfate

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About This Item

Empirical Formula (Hill Notation):

C₃₂H₂₉N₃O₇ · H₂SO₄

CAS Number:

212500-03-3

Molecular Weight:

665.67

UNSPSC Code:

41106305

PubChem Substance ID:

24278757

MDL number:

MFCD03453029

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assay

>99% (HPLC)

form

solid

color

white

solubility

DMSO: soluble 23 mg/mL, methanol: soluble 3.35 mg/mL, H₂O: insoluble

storage temp.

2-8°C

SMILES string

OS(O)(=O)=O.COC(=O)C1=C(c2cc(OC)c(OC)c(OC)c2)c3ccc(OCc4ccccn4)cc3C(=O)N1c5ccc(N)cc5

Gene Information

human ... PDE5A(8654)

Application

T-1032 has been used to study its effect on the inhibition of in vivo insulin functions in rats.

Biochem/physiol Actions

Potent specific inhibitor of phosphodiesterase V (PDE5). Potentiates nitric oxide/cGMP signaling pathway.

Potent specific inhibitor of phosphodiesterase V (PDE5). Shown to have potentiating effects on the nitric oxide/cGMP signaling pathway.

Preparation Note

T-1032 is soluble in DMSO at 23 mg/ml and is also soluble in methanol at 3.35 mg/ml. However, it is insoluble in water.

Storage Class

13 - Non Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number

011K4701

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Characterization and effects of methyl-2- (4-aminophenyl)-1, 2-dihydro-1-oxo-7- (2-pyridinylmethoxy)-4-(3,4, 5-trimethoxyphenyl)-3-isoquinoline carboxylate sulfate (T-1032), a novel potent inhibitor of cGMP-binding cGMP-specific phosphodiesterase (PDE5).

J Kotera et al.

Biochemical pharmacology, 60(9), 1333-1341 (2000-09-29)

An isoquinolone derivative, methyl-2-(4-aminophenyl)-1, 2-dihydro-1-oxo-7-(2-pyridinylmethoxy)-4-(3,4, 5-trimethoxyphenyl)-3-isoquinoline carboxylate sulfate (T-1032), was found to be a novel potent inhibitor of cyclic GMP (cGMP)-binding cGMP-specific phosphodiesterase (PDE5). We investigated the inhibitory effects of T-1032 on six PDE isozymes isolated from canine tissues. T-1032

Potentiation of penile tumescence by T-1032, a new potent and specific phosphodiesterase type V inhibitor, in dogs.

T Noto et al.

The Journal of pharmacology and experimental therapeutics, 294(3), 870-875 (2000-08-17)

We examined the mechanism underlying the potentiation of penile tumescence by methyl 2-(4-aminophenyl)-1, 2dihydro-1-oxo-7-(2-pyridinylmethoxy)-4-(3,4, 5-trimethoxyphenyl)3-isoquinoline carboxylate sulfate (T-1032), a new potent and selective phosphodiesterase type V inhibitor. In vivo, pelvic nerve stimulation induced a penile tumescence together with increase of

Pharmacological profile of T-1032, a novel specific phosphodiesterase type 5 inhibitor, in isolated rat aorta and rabbit corpus cavernosum.

M Takagi et al.

European journal of pharmacology, 411(1-2), 161-168 (2001-01-04)

This study was designed to examine the pharmacological properties of T-1032 (methyl-2-(4-aminophenyl)-1,2-dihydro-1-oxo-7-(2-pyridinylmethoxy)-4-(3,4,5-trimethoxyphenyl)-3-isoquinoline carboxylate sulfate), a novel phosphodiesterase type 5 inhibitor, in isolated rat aorta and rabbit corpus cavernosum. T-1032 (3x10(-11) to 3x10(-7) M) caused an endothelium-dependent relaxation in the isolated

T-1032, a cyclic GMP phosphodiesterase-5 inhibitor, acutely blocks physiologic insulin-mediated muscle haemodynamic effects and glucose uptake in vivo.

Hema Mahajan et al.

British journal of pharmacology, 140(7), 1283-1291 (2003-10-29)

1. Cyclic GMP phosphodiesterase-5 inhibitors have been shown to alter blood flow in specific tissues by potentiating local NO-dependent vasodilatory mechanisms. Since the haemodynamic effects of physiologic insulin, particularly capillary recruitment, may be critical for muscle glucose uptake in vivo