Zardaverine

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). 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 (Cay-21121), platelet-activating factor (PAF), collagen, arachidonic acid (Cay-90010, Cay-90010.1, Cay-10006607), or prostaglandin E1 (PGE1, Cay-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. 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).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: (Request formulation change), A crystalline solid. Solubility: DMSO: 100mM. lambdamax: 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.