货号:A218047
同义名:
米利酮
/ Win 47203; WIN 47,203
Milrinone是一种磷酸二酯酶 3(PDE3)抑制剂,IC50 为 56 nM,能够通过增加细胞内环磷酸腺苷(cAMP)水平改善心室功能,并引起血管舒张。
HazMat Fee + There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
| Type | HazMat fee for 500 gram (Estimated) |
| Excepted Quantity | USD 0.00 |
| Limited Quantity | USD 15-60 |
| Inaccessible (Haz class 6.1), Domestic | USD 80+ |
| Inaccessible (Haz class 6.1), International | USD 150+ |
| Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
| Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |


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|---|---|---|---|---|---|---|---|
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| 产品名称 | PDE ↓ ↑ | PDE1 ↓ ↑ | PDE10A ↓ ↑ | PDE2 ↓ ↑ | PDE3 ↓ ↑ | PDE4 ↓ ↑ | PDE5 ↓ ↑ | PDE6 ↓ ↑ | 其他靶点 | 纯度 | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Doxofylline | ✔ | 99+% | |||||||||||||||||
| Deltarasin |
+++
PDEδ , Kd: 38 nM |
95% | |||||||||||||||||
| 7-(2,3-Dihydroxypropyl)theophylline | ✔ | 98% | |||||||||||||||||
| Aminophylline |
+
PDE, IC50: 0.12 mM |
98+% | |||||||||||||||||
| Anagrelide HCl | ✔ | 99%+ | |||||||||||||||||
| Irsogladine | ✔ | AChR,mAChR | 99% | ||||||||||||||||
| PF-8380 |
+++
Autotaxin, IC50: 2.8 nM |
99%+ | |||||||||||||||||
| Dipyridamole | ✔ | 98% | |||||||||||||||||
| Balipodect |
++++
PDE10A, IC50: 0.3 nM |
99%+ | |||||||||||||||||
| Luteolin |
+
PDE1, Ki: 15.0 μM |
++
PDE2, Ki: 6.4 μM |
+
PDE3, Ki: 13.9 μM |
+
PDE4, Ki: 11.1 μM |
+
PDE5, Ki: 9.5 μM |
98% | |||||||||||||
| Milrinone |
++
PDE2, IC50: 5.2 μM |
++
PDE3, IC50: 2.1 μM |
ATPase | 99% | |||||||||||||||
| Pimobendan |
++
PDE3, IC50: 0.32 μM |
98% | |||||||||||||||||
| Cilostazol |
++
PDE3, IC50: 0.2 μM |
98% | |||||||||||||||||
| Fenspiride HCl |
+
PDE3, pIC50: 3.44 |
+
PDE4, pIC50: 4.16 |
99% (HPLC) | ||||||||||||||||
| (S)-(+)-Rolipram |
++
PDE4, IC50: 0.75 μM |
99% (HPLC) | |||||||||||||||||
| Apremilast |
+++
PDE4, IC50: 74 nM |
98% | |||||||||||||||||
| GSK256066 |
++++
PDE4B, IC50: 3.2 pM |
98+% | |||||||||||||||||
| Roflumilast |
++++
PDE4A1, IC50: 0.7 nM PDE4A4, IC50: 4.3 nM |
99% | |||||||||||||||||
| Rolipram |
+++
PDE4B, IC50: 130 nM |
99%+ | |||||||||||||||||
| Cilomilast |
+++
LPDE4, IC50: 100 nM HPDE4, IC50: 120 nM |
99% | |||||||||||||||||
| Avanafil |
++++
PDE5, IC50: 1 nM |
98% | |||||||||||||||||
| Vardenafil HCl Trihydrate |
++++
PDE5, IC50: 0.7 nM |
98% | |||||||||||||||||
| Tadalafil |
++++
PDE5, IC50: 1.8 nM |
98% | |||||||||||||||||
| Icariin |
++
PDE5, IC50: 0.432 μM |
98% | |||||||||||||||||
| Sildenafil | ✔ |
+++
PDE6, IC50: 33 nM |
98% | ||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | Cyclic nucleotide phosphodiesterases (PDEs) from the human heart were separated into three isoforms, FI, FII and FIII. Milrinone has been proved to be a potent and selective inhibitor of human cardiac FIII PDE, a "low Km" enzyme for cyclic AMP (cAMP-PDE). The IC50 value for the inhibition of FIII PDE was 0.42 μM, while those of FI and FII PDEs, "high Km" enzymes, were 38 and 19 μM, respectively[3]. The concentration of milrinone that produced 50% relaxation of tracheal spirals constricted by carbachol was 3.6 × 10-5 M; The IC50 for milrinone for lung parenchymal strips contracted by histamine was 3.2 × 10-5 M; Milrinone relaxed pulmonary artery rings constricted by norepinephrine with an IC50 of 3.8 × 10-6 M[4]. Milrinone caused a concentration-dependent increase in the cAMP level in rabbit and human platelets with similar potency. Furthermore, milrinone inhibited human platelet aggregation with an IC50 of 2 μM. It was a very potent cardiotonic agent, which concentration-dependently increased left ventricular developed pressure (LVDP) and contractility as well as cAMP in rabbit coronary smooth muscle cells[5]. In rabbit heart, partial inhibition of PDE4 by milrinone contributed to greater increases in cardiomyocyte cAMP and calcium levels[6]. In mongrel dogs underwent pulmonary artery catheterization, Milrinone led to significant increases in right ventricular function as well as significant improvements in pulmonary vascular resistance, pulmonary blood flow, and left ventricular filling[7]. |
| Concentration | Treated Time | Description | References | |
| Mouse denuded oocytes | 1.0 μM | Inhibition of oocyte maturation | J Clin Invest. 1998 Aug 1;102(3):532-7. | |
| Mouse oocytes | 1 µM | 2 hours | Maintain germinal vesicle stage arrest | J Cell Biol. 2017 Dec 4;216(12):3949-3957. |
| Murine tracheal epithelial cells | 13.7 µM | 80 minutes | To evaluate the effect of Milrinone on ciliary transport velocity in murine tracheal epithelial cells, results showed that Milrinone increased PTV in a dose-dependent manner with an EC50 of 13.7 µM. | Cells. 2025 Feb 5;14(3):228. |
| Adult mouse cardiomyocytes | 30 μM | 24 hours | To evaluate the effect of milrinone on hypoxia/reoxygenation or H2O2-induced cardiomyocyte apoptosis. Results showed that milrinone treatment significantly increased the apoptotic rate in both WT and TG cardiomyocytes. | J Mol Cell Cardiol. 2013 Nov;64:11-9. |
| HT22CREluc cells | 100 µM | ~11 hours | To investigate the effect of the PDE3-selective inhibitor milrinone on CRE-dependent transcriptional activity, results showed milrinone was effective at higher concentrations but two orders of magnitude less efficient than IBMX and rolipram. | Int J Mol Sci. 2020 Nov 17;21(22):8658. |
| HEK-TSHR cells | 1.0 mM | Milrinone, as a PDE3-specific inhibitor, exposed persistent TSHR-mediated cAMP signaling | Thyroid. 2013 Nov;23(11):1484-9. |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | DF508 mutant mice | Nasal perfusion | 100 μM | Single administration, lasting 4.5 minutes | To evaluate the effect of milrinone and forskolin combination on the potential difference across nasal epithelium in DF508 mutant mice. Results showed that the combination significantly increased the potential difference, indicating partial restoration of CFTR-mediated electrolyte transport. | Proc Natl Acad Sci U S A. 1997 Mar 18;94(6):2604-8 |
| Mice | HDM-driven allergic airway inflammation model | Intratracheal administration | 10 μg | 5 consecutive days | Study the effect of milrinone on allergic airway inflammation | JCI Insight. 2018 Jan 25;3(2):e94888. |
| Male ddY mice | LPS-induced microvascular permeability change model | Intraperitoneal injection | 5 – 10 mg/kg | Single dose, lasting 2 hours | Milrinone significantly inhibited LPS-induced dye leakage and elevation of serum TNF-α levels | Br J Pharmacol. 2001 May;133(2):237-42 |
| Mice | Murine tracheal model | Intratracheal administration | 13.7 µM | Single administration, lasting 80 minutes | To evaluate the effect of Milrinone on ciliary transport velocity in murine tracheae, results showed that Milrinone increased PTV via Ca2+ release from intracellular stores and depended on both PKA and PLC pathways. | Cells. 2025 Feb 5;14(3):228. |
| Mice | Transgenic mice with myocardial overexpression of PDE3A1 | Intraperitoneal injection | 10 mg/kg | Single dose | To evaluate the effect of milrinone on cardiac contractile function and heart rate. Results showed that milrinone treatment significantly attenuated the differences in cardiac contractile function and heart rate between TG and WT mice under ISO stimulation. | J Mol Cell Cardiol. 2013 Nov;64:11-9. |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02606253 | Heart Failure | Phase 4 | Active, not recruiting | October 31, 2018 | United States, Tennessee ... 展开 >> Vanderbilt University Medical Center Nashville, Tennessee, United States, 37204 收起 << |
| NCT02884011 | - | Completed | - | United States, Illinois ... 展开 >> Rush Univeristy Medical Center Chicago, Illinois, United States, 60612 收起 << | |
| NCT02261506 | Bacteremia | Not Applicable | Completed | - | Canada, Alberta ... 展开 >> Foothills Hospital Calgary, Alberta, Canada University of Alberta Hospital Edmonton, Alberta, Canada Canada, British Columbia Royal Columbian Hospital Vancouver, British Columbia, Canada St. Paul's Hospital Vancouver, British Columbia, Canada Canada, Manitoba St. Boniface Hospital Winnipeg, Manitoba, Canada Canada, Nova Scotia Queen Elizabeth II Hospital Halifax, Nova Scotia, Canada Canada, Ontario Kingston General Hospital Kingston, Ontario, Canada London Health Sciences Centre London, Ontario, Canada The Ottawa Hospital Ottawa, Ontario, Canada Sunnybrook Health Sciences Centre Toronto, Ontario, Canada, M4N3M5 Mount Sinai Hospital Toronto, Ontario, Canada St. Michael's Hospital Toronto, Ontario, Canada Toronto Western Hospital Toronto, Ontario, Canada Canada, Quebec CHUM Montreal, Quebec, Canada Université de Sherbrooke Sherbrooke, Quebec, Canada Canada Centre hospitalier affilié universitaire de Québec Quebec, Canada CSSS de Trois-Rivières Quebec, Canada 收起 << |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
4.73mL 0.95mL 0.47mL |
23.67mL 4.73mL 2.37mL |
47.34mL 9.47mL 4.73mL |
|
| CAS号 | 78415-72-2 |
| 分子式 | C12H9N3O |
| 分子量 | 211.22 |
| SMILES Code | N#CC1=CC(C2=CC=NC=C2)=C(C)NC1=O |
| MDL No. | MFCD00133539 |
| 别名 | 米利酮 ;Win 47203; WIN 47,203; Milrinone, Primacor, Corotrop, Milrila, Win-47203 |
| 运输 | 蓝冰 |
| InChI Key | PZRHRDRVRGEVNW-UHFFFAOYSA-N |
| Pubchem ID | 4197 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry,2-8°C |
| 溶解方案 |
DMSO: 50 mg/mL(236.72 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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