4-[[2-氟-3-[N'-(6-甲基吡啶-3-基)脲基]苯基]甲基]哌嗪-1-羧酸甲酯性質(zhì)、用途與生產(chǎn)工藝

生物活性

Omecamtiv mecarbil (CK-1827452)是一種特異性的心肌肌球蛋白激動劑，是用于左心室收縮性心臟衰竭的臨床藥物。Phase 2。

體外研究

In vitro, Omecamtiv mecarbil selectively activates cardiac myosin by increasing the myosin ATPase rate. In isolated cardiac myocytes, Omecamtiv mecarbil results in increase of myocyte contractility and overcomes of the myosin inhibitor BDM without increasing the calcium transient or inhibiting the PDE pathway.

體內(nèi)研究

Omecamtiv mecarbil significantly increases fractional shortening starting at 0.4 mM plasma concentrations in SD rats, sham animals and in rats with heart failure. In conscious dogs with myocardial infarction (MI-sHF), Omecamtiv mecarbil leads to a significant increase in wall thickening (25%), stroke volume (44%), cardiac output (22%) and left ventricular (LV) systolic ejection time (26%). In addition, Omecamtiv mecarbil also results in the decreases of some hemodynamic parameters including heart rate, mean left atrial pressure, and LV end-diastolic pressure. In conscious dogs with left ventricular hypertrophy (LVH-sHF), Omecamtiv mecarbil leads to similar and not statistically different effects on hemodynamic parameters.

生物活性

Omecamtiv mecarbil (CK-1827452)是一種特異性的心肌肌球蛋白激動劑，是用于左心室收縮性心臟衰竭的臨床藥物。Phase 2。

靶點

Target	Value
Myosin ATPase

體外研究

在體外，Omecamtiv mecarbil通過增加肌球蛋白ATPase比率，選擇性激活心肌肌球蛋白。 在離體心肌細胞中，Omecamtiv mecarbil導致肌細胞收縮性增加，并使肌漿球蛋白抑制劑BDM失效，而不增加鈣轉(zhuǎn)運或抑制PDE通路。

體內(nèi)研究

在SD大鼠，深水動物和心臟衰竭大鼠體內(nèi)，Omecamtiv mecarbil在血漿中濃度達到0.4 mM后顯著增加縮短分數(shù)。在清醒狀態(tài)下心肌梗死(MI-sHF)的狗體內(nèi)，Omecamtiv mecarbil顯著增加壁室厚度(25%)，每搏輸出量(44%)，心輸出量(22%)和左心室 (LV) 收縮射血時間(26%)。此外，Omecamtiv mecarbil也會導致一些血流動力學參數(shù)，包括心率，平均左房壓，和LV末期舒張壓下降。在左心室肥大(LVH-sHF)的清醒的狗體內(nèi)，Omecamtiv mecarbil對血流動力學參數(shù)具有類似且統(tǒng)計學差異化的影響。

4-[[2-氟-3-[N'-(6-甲基吡啶-3-基)脲基]苯基]甲基]哌嗪-1-羧酸甲酯 上下游產(chǎn)品信息

上游原料

下游產(chǎn)品

4-[[2-氟-3-[N'-(6-甲基吡啶-3-基)脲基]苯基]甲基]哌嗪-1-羧酸甲酯 試劑級價格

更新日期	產(chǎn)品編號	產(chǎn)品名稱	CAS編號	包裝	價格
2025/02/08	HY-14233	4-[[2-氟-3-[N'-(6-甲基吡啶-3-基)脲基]苯基]甲基]哌嗪-1-羧酸甲酯 Omecamtiv mecarbil	873697-71-3	1 mg	389元
2025/02/08	HY-14233	4-[[2-氟-3-[N'-(6-甲基吡啶-3-基)脲基]苯基]甲基]哌嗪-1-羧酸甲酯 Omecamtiv mecarbil	873697-71-3	10mM * 1mLin DMSO	883元

4-[[2-氟-3-[N'-(6-甲基吡啶-3-基)脲基]苯基]甲基]哌嗪-1-羧酸甲酯 生產(chǎn)廠家

 

873697-71-3, 4-[[2-氟-3-[N'-(6-甲基吡啶-3-基)脲基]苯基]甲基]哌嗪-1-羧酸甲酯 相關(guān)搜索:

• Inhibitors
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• C20H24FN5O3
• 化合物OMECAMTIV MECARBIL,10 MM DMSO 溶液
• OMECAMTIV MECARBIL (CK-1827452),心肌肌球蛋白激動劑
• 化合物OMECAMTIV MECARBIL
• MYOSIN激活劑(OMECAMTIV MECARBIL)
• 4-[[2-氟-3-[N'-(6-甲基吡啶-3-基)脲基]苯基]甲基]哌嗪-1-羧酸甲酯
• 873697-71-3
• Omecamtiv mecarbil, 10 mM in DMSO
• 1-Piperazinecarboxylic acid,4-[[2-fluoro-3-[[[(6-methyl-3-py...
• OMecaMtiv Mecarbil USP/EP/BP
• Omecamtiv mecarbil?, >98%
• CK1827452, >98%
• CS-827
• CK-1827452; CK1827452;CK 1827452
• CK 1827452 - Omecamtiv Mecarbil | CK-452
• OMECAMTIV MECARBIL (CK-1827452);CK1827452
• methyl 4-[(2-fluoro-3-{[(6-methylpyridin-3-yl)carbamoyl]amino}phenyl)methyl] piperazine-1-carboxylate
• Methyl 4-[[2-fluoro-3-[N'-(6-methylpyridin-3-yl)ureido]phenyl]methyl]piperazine-1-carboxylate Omecamtiv mecarbil(CK1827452)
• methyl 4-(2-fluoro-3-(3-(6-methylpyridin-3-yl)ureido)benzyl)piperazine-1-carboxylate
• Methyl 4-[[2-fluoro-3-[N'-(6-methylpyridin-3-yl)ureido]phenyl]methyl]piperazine-1-carboxylate
• mecamtiv mecarbil
• CK 1827452O
• CK-1827452 (OMecaMtiv Mecarbil)
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• OMecaMtiv Mecarbil (CK-1827452)
• OMecaMtiv Mecarbil
• 1-Piperazinecarboxylic acid,4-[[2-fluoro-3-[[[(6-methyl-3-pyridinyl)amino]carbonyl]amino]phenyl]methyl]-, methyl ester