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Siguazodan

Catalog No. T12913 CAS 115344-47-3

Synonyms: SKF 94836

Siguazodan (SKF 94836) is an effective, selective, orally active phosphodiesterase III ((PDE-III)) inhibitor with an IC50 of 117 nM. Siguazodan inhibited phenylephrine induced 5-HT release with an IC50 value of 4.2 μM。 Siguazodan can increase cAMP accumulation in intact platelets, with EC50 of 18.88 μM。

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Siguazodan, CAS 115344-47-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 135.00
5 mg	In stock	$ 289.00
10 mg	In stock	$ 455.00
25 mg	In stock	$ 753.00
50 mg	In stock	$ 1,060.00
100 mg	In stock	$ 1,430.00
500 mg	In stock	$ 2,860.00
1 mL * 10 mM (in DMSO)	In stock	$ 429.00

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Purity: 99.77%

Purity: 99.63%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Siguazodan (SKF 94836) is an effective, selective, orally active phosphodiesterase III ((PDE-III)) inhibitor with an IC50 of 117 nM. Siguazodan inhibited phenylephrine induced 5-HT release with an IC50 value of 4.2 μM。 Siguazodan can increase cAMP accumulation in intact platelets, with EC50 of 18.88 μM。
Targets&IC50	PDE3:117 nM
In vitro	the major cyclic AMP-hydrolysing PDE in human platelet supernatantsselectively inhibited by Siguazodan . The inhibited enzyme has been variously termed cyclic GMP-inhibited PDE or PDE-III. In platelet-rich plasma (PRP), Siguazodan inhibits U46619-induced aggregation more potently than that induced by adenosine 5'-diphosphate (ADP), and collagen. In washed platelets, Siguazodan increases cyclic AMP levels and reduces cytoplasmic free calcium. ADP decreases the ability of Siguazodan to raise cyclic AMP and this may explain its lower potency in inhibiting responses to ADP. Siguazodan has anti-platelet actions over the same concentration range that it is an inotrope and vasodilator[2].
In vivo	Siguazodan is a selective phosphodiesterase III inhibitor that has positive inotropic and vasodilating actions in various laboratory animals and is orally active with a long duration of action in conscious dogs[2].

Synonyms	SKF 94836
Molecular Weight	284.32
Formula	C14H16N6O
CAS No.	115344-47-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (175.86 mM)

References and Literature

1. Murray KJ, et al. The effects of siguazodan, a selective phosphodiesterase inhibitor, on human platelet function. Br J Pharmacol. 1990 Mar;99(3):612-6. 2. Freitag A, et al. Phosphodiesterase inhibitors suppress alpha2-adrenoceptor-mediated 5-hydroxytryptamine release from tracheae of newborn rabbits. Eur J Pharmacol. 1998 Jul 31;354(1):67-71. 3. Tang KM, et al. Photoaffinity labelling of cyclic GMP-inhibited phosphodiesterase (PDE III) in human and rat platelets and rat tissues: effects of phosphodiesterase inhibitors. Eur J Pharmacol. 1994 Jun 15;268(1):105-14.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compound Library Cuproptosis Compound Library ReFRAME Related Library Bioactive Compounds Library Max Human Metabolite Library Orally Active Compound Library Metabolism Compound Library

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Keywords

Siguazodan 115344-47-3 Metabolism PDE SKF94836 inhibit Phosphodiesterase (PDE) SKF 94836 Inhibitor SKF-94836 inhibitor

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