1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. Siguazodan

Siguazodan (Synonyms: SKF 94836)

Cat. No.: HY-19026 Purity: >99.0%
Handling Instructions

Siguazodan (SKF 94836) is a potent, selective and orally active phosphodiesterase III (PDE-III) inhibitor with an IC50 of 117 nM. Siguazodan increases cAMP accumulation in intact platelets with an EC50 of 18.88 μM. Siguazodan also inhibits phenylephrine-induced 5-HT release with an IC50 value of 4.2 μM.

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Siguazodan Chemical Structure

Siguazodan Chemical Structure

CAS No. : 115344-47-3

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10 mM * 1 mL in DMSO USD 375 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
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Description

Siguazodan (SKF 94836) is a potent, selective and orally active phosphodiesterase III (PDE-III) inhibitor with an IC50 of 117 nM. Siguazodan increases cAMP accumulation in intact platelets with an EC50 of 18.88 μM. Siguazodan also inhibits phenylephrine-induced 5-HT release with an IC50 value of 4.2 μM[1][2][3].

IC50 & Target

IC50: 117 nM (phosphodiesterase III)[1]

In Vitro

Siguazodan selectively inhibits the major cyclic AMP-hydrolysing PDE in human platelet supernatants. 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. Treatment of the PRP with Aspirin has no effect on the potency of Siguazodan. 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 potent, selective inhibitor of phosphodiesterase III 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].

Molecular Weight

284.32

Formula

C₁₄H₁₆N₆O

CAS No.

115344-47-3

SMILES

O=C1CC(C)C(C2=CC=C(/N=C(NC)/NC#N)C=C2)=NN1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >99.0%

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Keywords:

SiguazodanSKF 94836SKF94836SKF-94836Phosphodiesterase (PDE)Inhibitorinhibitorinhibit

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