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米力农 /Milrinone 99%+

货号:A218047 同义名: 米利酮 / Win 47203;WIN 47,203 Ambeed 开学季,买赠积分,赢豪礼

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.

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+
Milrinone 化学结构 CAS号:78415-72-2
Milrinone 化学结构
CAS号:78415-72-2
Milrinone 3D分子结构
CAS号:78415-72-2
Milrinone 化学结构 CAS号:78415-72-2
Milrinone 3D分子结构 CAS号:78415-72-2
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Milrinone 纯度/质量文件 产品仅供科研

货号:A218047 标准纯度: 99%+
批次查询: 批次纯度:

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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

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。

Milrinone 生物活性

靶点
  • PDE2

    PDE2, IC50:5.2 μM

  • PDE3

    PDE3, IC50:2.1 μM

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].

Milrinone 临床研究

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 <<

Milrinone 参考文献

[1]Cone J, Wang S, et al. Comparison of the effects of cilostazol and milrinone on intracellular cAMP levels and cellular function in platelets and cardiac cells. J Cardiovasc Pharmacol. 1999 Oct;34(4):497-504.

[2]Shipley JB, Tolman D, et al. Milrinone: basic and clinical pharmacology and acute and chronic management. Am J Med Sci. 1996 Jun;311(6):286-91.

[3]Ito M, Tanaka T, Saitoh M, Masuoka H, Nakano T, Hidaka H. Selective inhibition of cyclic AMP phosphodiesterase from various human tissues by milrinone, a potent cardiac bipyridine. Biochem Pharmacol. 1988 May 15;37(10):2041-4. doi: 10.1016/0006-2952(88)90554-0. PMID: 2837222.

[4]Rossing TH, Drazen JM. Effects of milrinone on contractile responses of guinea pig trachea, lung parenchyma and pulmonary artery. J Pharmacol Exp Ther. 1986 Sep;238(3):874-9. PMID: 3746666.

[5]Cone J, Wang S, Tandon N, Fong M, Sun B, Sakurai K, Yoshitake M, Kambayashi J, Liu Y. Comparison of the effects of cilostazol and milrinone on intracellular cAMP levels and cellular function in platelets and cardiac cells. J Cardiovasc Pharmacol. 1999 Oct;34(4):497-504. doi: 10.1097/00005344-199910000-00004. PMID: 10511123.

[6]Shakur Y, Fong M, Hensley J, Cone J, Movsesian MA, Kambayashi J, Yoshitake M, Liu Y. Comparison of the effects of cilostazol and milrinone on cAMP-PDE activity, intracellular cAMP and calcium in the heart. Cardiovasc Drugs Ther. 2002 Sep;16(5):417-27. doi: 10.1023/a:1022186402442. PMID: 12652111.

[7]Chen EP, Bittner HB, Davis RD Jr, Van Trigt P 3rd. Milrinone improves pulmonary hemodynamics and right ventricular function in chronic pulmonary hypertension. Ann Thorac Surg. 1997 Mar;63(3):814-21. doi: 10.1016/s0003-4975(97)00011-8. PMID: 9066407.

Milrinone 实验方案

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

Milrinone 技术信息

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

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