product name Milrinone
Description: Milrinone (also known as Win 47203) is a potent phosphodiesterase 3 (PDE3) inhibitor that is used to increase the hearts contractility. Milrinone has shown the effect of concentration-dependent inhibition of PDE3 on the photolabelling with a IC50 value of 56±12nM. In addition, Milrinone has been reported to increase the accumulation of [3H] cAMP with a EC50 value of 5329±970nM in platelets.
References: J Cardiovasc Pharmacol. 1999 Oct;34(4):497-504; Br J Pharmacol. 1996 Oct;119(3):609-15.
211.22
Formula
C12H9N3O
CAS No.
78415-72-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 42 mg/mL (198.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
Win 47203
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19399531
| In Vitro |
In vitro activity: Milrinone causes a concentration-dependent increase in the cAMP level in rabbit and human platelets with similar potency. Milrinone inhibits human platelet aggregation with a median inhibitory concentration (IC50) of 2 mM.Milrinone concentration-dependently increases left ventricular developed pressure (LVDP) and contractility. Milrinone concentration-dependently increases cAMP in rabbit coronary smooth muscle cells. Milrinone increases intracellular cyclic adenosine monophosphate by inhibiting Type III phosphodiesterase. Milrinone is a potent (IC50 = 0.16-0.90 mM) and selective (100 times peak III relative to peak I) peak III inhibitor. Milrinone significant increases in cAMP content accompany significant vasorelaxation. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Milrinone inhibits PDE4 in addition to PDE3 activity in the rabbit heart. Milrinone (>10 microM) causes greater elevations in intracellular cAMP and calcium than cilostazol. Milrinone causes similar increases in heart rate, cardiac output, and left ventricular +dP/dt and decreases in end-diastolic pressure and systemic vascular resistance in anaesthetized dogs. Milrinone leads to significant increases in right ventricular function as well as significant improvements in pulmonary vascular resistance, pulmonary blood flow, and left ventricular filling in mongrel dogs underwent pulmonary artery catheterization. |
| Animal model | Rabbit |
| Formulation & Dosage | |
| References | J Cardiovasc Pharmacol. 1999 Oct;34(4):497-504; Br J Pharmacol. 1996 Oct;119(3):609-15. |
Related Posts
product name Milrinone
Description: Milrinone (also known as Win 47203) is a potent phosphodiesterase 3 (PDE3) inhibitor that is used to increase the hearts contractility. Milrinone has shown the effect of concentration-dependent inhibition of PDE3 on the photolabelling with a IC50 value of 56±12nM. In addition, Milrinone has been reported to increase the accumulation of [3H] cAMP with a EC50 value of 5329±970nM in platelets.
References: J Cardiovasc Pharmacol. 1999 Oct;34(4):497-504; Br J Pharmacol. 1996 Oct;119(3):609-15.
211.22
Formula
C12H9N3O
CAS No.
78415-72-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 42 mg/mL (198.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
Win 47203
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19399531
| In Vitro |
In vitro activity: Milrinone causes a concentration-dependent increase in the cAMP level in rabbit and human platelets with similar potency. Milrinone inhibits human platelet aggregation with a median inhibitory concentration (IC50) of 2 mM.Milrinone concentration-dependently increases left ventricular developed pressure (LVDP) and contractility. Milrinone concentration-dependently increases cAMP in rabbit coronary smooth muscle cells. Milrinone increases intracellular cyclic adenosine monophosphate by inhibiting Type III phosphodiesterase. Milrinone is a potent (IC50 = 0.16-0.90 mM) and selective (100 times peak III relative to peak I) peak III inhibitor. Milrinone significant increases in cAMP content accompany significant vasorelaxation. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Milrinone inhibits PDE4 in addition to PDE3 activity in the rabbit heart. Milrinone (>10 microM) causes greater elevations in intracellular cAMP and calcium than cilostazol. Milrinone causes similar increases in heart rate, cardiac output, and left ventricular +dP/dt and decreases in end-diastolic pressure and systemic vascular resistance in anaesthetized dogs. Milrinone leads to significant increases in right ventricular function as well as significant improvements in pulmonary vascular resistance, pulmonary blood flow, and left ventricular filling in mongrel dogs underwent pulmonary artery catheterization. |
| Animal model | Rabbit |
| Formulation & Dosage | |
| References | J Cardiovasc Pharmacol. 1999 Oct;34(4):497-504; Br J Pharmacol. 1996 Oct;119(3):609-15. |