An inhibitor of PDE3 (IC50s = 0.45 and 1 µM for PDE3A and PDE3B

Milrinone – 100 mg

Brand:
Cayman
CAS:
78415-72-2
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Milrinone is an inhibitor of type 3 phosphodiesterases (PDEs), inhibiting recombinant PDE3A and PDE3B with IC50 values of 0.45 and 1 μM, respectively.{19198} It is selective for PDE3 over PDE1, PDE2, PDE4, PDE5, and PDE7 (IC50s = 263, >300, 17.5, 49.1, and 58.3 μM, respectively).{19198} Milrinone (0.1-1 mg/kg) has positive inotropic effects, increasing cardiac contractile force in anesthetized dogs with a concomitant increase in heart rate but not blood pressure.{42416} It also increases contractile force in models of propranolol- and verapamil-induced heart failure in anesthetized dogs when administered at an initial dose of 30 µg/kg followed by a continuous 3 µg/kg per minute infusion. Milrinone has vasodilatory effects as well, decreasing mean aortic pressure and increasing venous compliance in anesthetized dogs when administered at an initial dose of 10 µg/kg followed by a continuous 1.7-2.4 µg/kg per minute infusion.{42417} Formulations containing milrinone have been used in the treatment of heart failure.  

 

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Description

An inhibitor of PDE3 (IC50s = 0.45 and 1 µM for PDE3A and PDE3B, respectively); selective for PDE3 over PDE1, PDE2, PDE4, PDE5, and PDE7 (IC50s = 263, >300, 17.5, 49.1, and 58.3 μM, respectively); increases contractile force in anesthetized dogs at 0.1-1 mg/kg; increases contractile force in models of propranolol- and verapamil-induced heart failure in anesthetized dogs at 30 µg/kg followed by a 3 µg/kg infusion; decreases mean aortic pressure and increases venous compliance in anesthetized dogs at 10 µg/kg followed by a 1.7-2.4 µg/kg per minute infusion

Formal name: 1,6-dihydro-2-methyl-6-oxo-[3,4′-bipyridine]-5-carbonitrile

Synonyms:  WIN 47,203

Molecular weight: 211.2

CAS: 78415-72-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phosphodiesterases||Research Area|Cardiovascular System|Cardiovascular Diseases|Heart Failure||Research Area|Cardiovascular System|Heart|Arrhythmia||Research Area|Cardiovascular System|Heart|Myocardial Contractility||Research Area|Cardiovascular System|Vasculature|Vasodilation||Research Area|Cell Biology|Cell Signaling|cGMP Signaling

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