A PDE3 inhibitor
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Siguazodan

Item No. 46199

Technical Information
Formal Name
N-cyano-N-methyl-N′-[4-(1,4,5,6-tetrahydro-4-methyl-6-oxo-3-pyridazinyl)phenyl]-guanidine
CAS Number
115344-47-3
Synonyms
  • SKF 94836
Molecular Formula
C14H16N6O
Formula Weight
Purity
≥98%
A solid
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
CNC(NC#N)=NC1=CC=C(C=C1)C(C(C2)C)=NNC2=O
InChi Code
InChI=1S/C14H16N6O/c1-9-7-12(21)19-20-13(9)10-3-5-11(6-4-10)18-14(16-2)17-8-15/h3-6,9H,7H2,1-2H3,(H,19,21)(H2,16,17,18)
InChi Key
NUHPODZZKHQQET-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Siguazodan is a phosphodiesterase 3 (PDE3) inhibitor (IC50 = 0.84 µM for the human platelet enzyme).1 It inhibits U-46619-, ADP-, or collagen-induced platelet aggregation in isolated human platelet-rich plasma (IC50s = 1.8, 4, and 6.9 µM, respectively). Siguazodan (30 µM) induces relaxation and increases PKA activity in methacholine- or histamine-precontracted dog trachealis strips.2 It also potentiates isoproterenol- or sodium nitroprusside-induced relaxation in dog trachealis strips. Siguazodan has positive inotropic and vasodilator activity with minimal effects on blood pressure and heart rate in anesthetized cats and dogs.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Patnaik, D., Pao, P.-C., Zhao, W.-N., et al. Exifone is a potent HDAC1 activator with neuroprotective activity in human neuronal models of neurodegeneration. ACS Chem. Neurosci. 12(2), 271-284 (2021).

    2. Torphy, T.J., Burman, M., Huang, L.B.F., et al. Inhibition of the low km cyclic AMP phosphodiesterase in intact canine trachealis by SK&F 94836: Mechanical and biochemical responses. J. Pharmacol Exp. Ther. 246(3), 843-850 (1988).

    3. Gristwood, R.W., Comer, M.B., Eden, R.J., et al. In vivo pharmacological studies with SK&F 94836, a potent inotrope/vasodilator with a sustained duration of action. Br. J. Pharmacol. 93(4), 893-901 (1988).