货号:A218047
同义名:
米利酮
/ Win 47203;WIN 47,203
Milrinone is a phosphodiesterase 3 (PDE3) inhibitor with IC50 of 56 nM, it increases intracellular cyclic adenosine monophosphate resulting in improved ventricular function and vasodilation.
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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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技术支持
免费溶解
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 |
99+% | |||||||||||||||||
7-(2,3-Dihydroxypropyl)theophylline | ✔ | 99%+ | |||||||||||||||||
Aminophylline |
+
PDE, IC50: 0.12 mM |
99%+ | |||||||||||||||||
Anagrelide HCl | ✔ | 99%+ | |||||||||||||||||
Irsogladine | ✔ | mAChR,AChR | 99%+ | ||||||||||||||||
PF-8380 |
+++
Autotaxin, IC50: 2.8 nM |
99%+ | |||||||||||||||||
Dipyridamole | ✔ | 99%+ | |||||||||||||||||
Balipodect |
++++
PDE10A, IC50: 0.3 nM |
99%+ | |||||||||||||||||
PF-2545920 |
++++
PDE10A, IC50: 0.37 nM |
97% | |||||||||||||||||
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 |
99%+ | |||||||||||||||||
Cilostazol |
++
PDE3, IC50: 0.2 μM |
99%+ | |||||||||||||||||
Fenspiride HCl |
+
PDE3, pIC50: 3.44 |
+
PDE4, pIC50: 4.16 |
99%+ | ||||||||||||||||
(S)-(+)-Rolipram |
++
PDE4, IC50: 0.75 μM |
98% | |||||||||||||||||
Apremilast |
+++
PDE4, IC50: 74 nM |
98% | |||||||||||||||||
GSK256066 |
++++
PDE4B, IC50: 3.2 pM |
98+% | |||||||||||||||||
Roflumilast |
++++
PDE4A4, IC50: 4.3 nM PDE4A1, IC50: 0.7 nM |
99% | |||||||||||||||||
Rolipram |
+++
PDE4B, IC50: 130 nM |
99%+ | |||||||||||||||||
Cilomilast |
+++
LPDE4, IC50: 100 nM HPDE4, IC50: 120 nM |
98+% | |||||||||||||||||
Avanafil |
++++
PDE5, IC50: 1 nM |
99%+ | |||||||||||||||||
Vardenafil HCl Trihydrate |
++++
PDE5, IC50: 0.7 nM |
99%+ | |||||||||||||||||
Tadalafil |
++++
PDE5, IC50: 1.8 nM |
98% | |||||||||||||||||
Icariin |
++
PDE5, IC50: 0.432 μM |
98% | |||||||||||||||||
Sildenafil | ✔ |
+++
PDE6, IC50: 33 nM |
99%+ | ||||||||||||||||
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]. |
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 |
别名 | 米利酮 ;Win 47203;WIN 47,203;Milrinone, Primacor, Corotrop, Milrila, Win-47203 |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
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 |
动物实验配方 |