A dual inhibitor of PDE3 and PDE4 (IC50s = 0.617 and 1.738 μM

Zardaverine – 5 mg

Brand:
Cayman
CAS:
101975-10-4
Storage:
-20
UN-No:
Non-Hazardous - /

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).{46697} 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.{46698} 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).{46699}  

 

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Description

A dual inhibitor of PDE3 and PDE4 (IC50s = 0.617 and 1.738 μM, respectively, for the rat cardiac ventricle enzymes); selective for PDE3 and PDE4 over PDE1B, PDE2, and PDE5 (IC50s = >138 μM for all); inhibits aggregation of human platelets induced by ADP, PAF, collagen, arachidonic acid, or PGE1 and ADP (IC50s = 1.5-16.2 μM); inhibits zymosan-induced superoxide anion release from human PMNs (IC50 = 0.4 μM); decreases lung resistance and increases dynamic compliance in a rat model of acetylcholine-induced bronchospasm at 10 μmol/kg; decreases the viability of HeLa, COLO 741, NCI H2122, and A2058 cells (IC50s = 0.032, 0.027, 0.26, and 0.13 μM, respectively)

Formal name: 6-[4-(difluoromethoxy)-3-methoxyphenyl]-3(2H)-pyridazinone

Synonyms: 

Molecular weight: 268.2

CAS: 101975-10-4

Purity: ≥98%

Formulation: A crystalline solid

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