1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)

Milrinone (Synonyms: Win 47203)

Cat. No.: HY-14252 Purity: 99.78%
Data Sheet SDS Handling Instructions

Milrinone is a PDE3 inhibitor, and also an inotrope and vasodilator.

For research use only. We do not sell to patients.
Milrinone Chemical Structure

Milrinone Chemical Structure

CAS No. : 78415-72-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $55 In-stock
50 mg $50 In-stock
100 mg $79 In-stock
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Description

Milrinone is a PDE3 inhibitor, and also an inotrope and vasodilator.

In Vitro

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[1]. 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[4].

In Vivo

Milrinone (1 μg/kg/min, i.v.) significantly reduces PAP, PVR (−18.96 ± 1.7%), and LAP (−26.03 ± 2.3%) in congestive heart failure (CHF) rats. Milrinone (1 mg/mL, inhalation) results in a near-maximal reduction of PAP without significant effects on AP, decreases pulmonary artery pressure similarly in a larger collective of CHF rats. Milrinone inhalation selectively increases cAMP but not cGMP plasma concentrations in both groups. Repeated milrinone inhalations even reduce lung wet/dry weight ratio[2]. Milrinone (49.5 μg) largely shifts the ESPVR upwards and significantly increases end-systolic pressure (ESP(0.08)) and the systolic pressure-volume area (PVA(0.08)) at a mid-range LV volume (0.08 mL/g myocardium). Milrinone also slightly decreases LV ESP(ESV) and decreased Ea[3].

Clinical Trial
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References
Preparing Stock Solutions
Concentration Volume Mass 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
Please refer to the solubility information to select the appropriate solvent.
Animal Administration
[2]

Milrinone is formulated in 0.9% NaCl.

In juvenile rats of 100 ± 8 g body weight (bw), CHF is induced by supracoronary aortic banding. In brief, rats are anesthetized by intraperitoneal injection of ketamine (87 mg/kg bw) and xylazine (13 mg/kg bw). Rats are placed in the supine position, the chest wall is shaved, and a left thoracotomy is performed in the third intercostal space during ventilation with 100% O2. The ascending aorta is freed from connective tissue and partially occluded by implantation of a titanium clip with a defined internal diameter of 0.8 mm. After surgical closure of the thorax, the rats are allowed to recover from anesthesia. For postoperative analgesia, rats receive 250 mg/kg bw of metamizole intramuscularly immediately after the operation and on the first postoperative day. Sham-operated rats serve as controls. After recovery from anesthesia, the animals are placed in cages with free access to water and standard laboratory diet. For inhalation, milrinone (0.2-5 mg/mL) or NaCl (0.9%) are nebulized using an ultrasonic nebulizer and inhaled for 3 min at identical peak inspiratory pressures as used throughout the experiment. A 3-min nebulization of 1 mg/mL milrinone results in vaporization of 14 μg of the phosphodiesterase-3 inhibitor as determined by microgravimetry. Therefore, the respective dose of 39 μg/kg is analog to inhaled doses in human studies. For intravenous delivery, milrinone (initial bolus of 2-10 μg/kg, followed by 0.2-1 μg/kg/min) or equivalent volumes of NaCl (0.9%; initial bolus of 1.6 mL/kg, followed by 10 μL/kg/h) are administered by an infusion pump for 10 min. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

211.22

Formula

C₁₂H₉N₃O

CAS No.

78415-72-2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 46 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Milrinone
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