A dual inhibitor of PDE3 and PDE4
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Zardaverine

Item No. 29685

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[4-(difluoromethoxy)-3-methoxyphenyl]-3(2H)-pyridazinone
CAS Number
101975-10-4
Molecular Formula
C12H10F2N2O3
Formula Weight
268.2
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 100mM
λmax
255 nm
SMILES
FC(F)OC1=CC=C(C2=NNC(C=C2)=O)C=C1OC
InChi Code
InChI=1S/C12H10F2N2O3/c1-18-10-6-7(2-4-9(10)19-12(13)14)8-3-5-11(17)16-15-8/h2-6,12H,1H3,(H,16,17)
InChi Key
HJMQDJPMQIHLPB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $110

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    10 mg

    $186

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    25 mg

    $420

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    Product Description

    Zardaverine is a dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 (IC50s = 0.617 and 1.738 μM, respectively, for the rat cardiac ventricle enzymes).1 It is selective for PDE3 and PDE4 over PDE1B, PDE2, and PDE5 (IC50s = >138 μM for all). Zardaverine inhibits aggregation of human platelets induced by ADP (Item No. 21121), platelet-activating factor (PAF), collagen, arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607), or prostaglandin E1 (PGE1; Item No. 13010) and ADP (IC50s = 1.5-16.2 μM). It inhibits zymosan-induced superoxide anion release from human polymorphonuclear (PMN) cells (IC50 = 0.4 μM). Zardaverine (10 μmol/kg) decreases lung resistance and increases dynamic compliance in a rat model of acetylcholine-induced bronchospasm.2 It decreases the viability of HeLa, COLO 741, NCI H2122, and A2058 cells that endogenously express high levels of PDE3A (IC50s = 0.032, 0.027, 0.26, and 0.13 μM, respectively), but is inactive against a panel of eight cancer cell lines that express low levels of PDE3A (IC50s = >16 μM for all).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schudt, C., Winder, S., Müller, B., et al. Zardaverine as a selective inhibitor of phosphodiesterase isozymes. Biochem. Pharmacol. 42(1), 153-162 (1991).

    2. Hoymann, H.G., Heinrich, U., Beume, R., et al. Comparative investigation of the effects of zardaverine and theophylline on pulmonary function in rats. Exp. Lung Res. 20(3), 235-250 (1994).

    3. Nazir, M., Senkowski, W., Nyberg, F., et al. Targeting tumor cells based on phosphodiesterase 3A expression. Exp. Cell Res. 361(2), 308-315 (2017).