| CAS NO: | 78415-72-2 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| 5g | 电议 |
| 10g | 电议 |
| Molecular Weight (MW) | 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 | |
| Other info | Chemical Name: 6-methyl-2-oxo-5-pyridin-4-yl-1H-pyridine-3-carbonitrile InChi Key: PZRHRDRVRGEVNW-UHFFFAOYSA-N InChi Code: InChI=1S/C12H9N3O/c1-8-11(9-2-4-14-5-3-9)6-10(7-13)12(16)15-8/h2-6H,1H3,(H,15,16) SMILES Code: N#CC1=CC(C2=CC=NC=C2)=C(C)NC1=O |
| Synonyms | Win 47203; Win47203; Milrinone, Primacor, Corotrop, Milrila, Win-47203 |
| 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: Milrinone (1 μM) increases PKA activity in hypoxic myocytes to normoxic levels. Milrinone (50 nM) normalizes TP receptor sensitivity in hypoxic myocytes by restoring PKA-mediated regulatory TP receptor phosphorylation. Milrinone significantly reduces NE-induced vasoconstriction, attenuating both NE sensitivity and maximal tension generation. Inhibition of ATP-sensitive K+ channels or voltage-gated K+ channels do not prevent the milrinone-induced attenuation of NE responses |
|---|---|
| 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 | >10 microM |
| References | J Cardiovasc Pharmacol. 1999 Oct;34(4):497-504; Br J Pharmacol. 1996 Oct;119(3):609-15. |
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