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Purity: ≥98%
Milrinone (formerly known as Win-47203; Win 47203; trade name Primacor) is a potent and selective phosphodiesterase 3 (PDE3) inhibitor that is used as a pulmonary vasodilator to increase the heart's 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.
| ln Vitro |
PKA activity in hypoxic myocytes is raised to normoxic levels by 1 µM milrinone. By reinstating PKA-mediated regulatory TP receptor phosphorylation, milrinone (50 nM) restores TP receptor sensitivity in hypoxic myocytes[1]. Milrinone attenuates maximal tension generation and NE sensitivity by substantially reducing NE-induced vasoconstriction. Milrinone-induced attenuation of NE responses is not prevented by voltage-gated or ATP-sensitive K+ channel inhibition[4].
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| ln Vivo |
In rats with congestive heart failure (CHF), milrinone (1 μg/kg/min, iv) dramatically lowers PAP, PVR (−18.96 ± 1.7%), and LAP (−26.03 ± 2.3%). Inhaling 1 mg/mL of milrinone reduces PAP almost to its near-maximum without having a substantial impact on AP. A bigger group of CHF rats also experience a comparable decrease in pulmonary artery pressure. In both groups, inhaling milrinone selectively raises the amounts of cAMP but not cGMP in the plasma. Milrinone inhalations repeated over time even lower the ratio of lung wet to dry weight[2]. At a mid-range LV volume (0.08 mL/g myocardium), milrinone (49.5 μg) considerably raises the systolic pressure-volume area (PVA(0.08)) and end-systolic pressure (ESP(0.08)). It also moves the ESPVR upward. Additionally, mildrinone modestly reduces Ea and LV ESP(ESV)[3].
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| References |
[1]. Santhosh KT, et al. Milrinone attenuates thromboxane receptor-mediated hyperresponsiveness in hypoxic pulmonary arterial myocytes. Br J Pharmacol. 2011 Jul;163(6):1223-36.
[2]. Hentschel T, et al. Inhalation of the phosphodiesterase-3 inhibitor milrinone attenuates pulmonary hypertension in a rat model of congestive heart failure. Anesthesiology. 2007 Jan;106(1):124-31. [3]. Kishi T, et al. Effects of milrinone on left ventricular end-systolic pressure-volume relationship of rat hearts in situ. Clin Exp Pharmacol Physiol. 2001 Sep;28(9):737-42. [4]. Taylor MS, et al. Effect of milrinone on small mesenteric artery vasoconstriction: role of K(+) channels. Am J Physiol. 1999 Jul;277(1 Pt 1):G69-78 |
| Molecular Formula |
C12H9N3O
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| Molecular Weight |
211.22
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| CAS # |
78415-72-2
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| Related CAS # |
Milrinone lactate;100286-97-3;Milrinone-d3;2749393-50-6
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| SMILES |
O=C1C(C#N)=C([H])C(C2C([H])=C([H])N=C([H])C=2[H])=C(C([H])([H])[H])N1[H]
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| InChi Key |
PZRHRDRVRGEVNW-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
6-methyl-2-oxo-5-pyridin-4-yl-1H-pyridine-3-carbonitrile
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.7344 mL | 23.6720 mL | 47.3440 mL | |
| 5 mM | 0.9469 mL | 4.7344 mL | 9.4688 mL | |
| 10 mM | 0.4734 mL | 2.3672 mL | 4.7344 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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