化合物Omecamtiv mecarbil T2006

Product Introduction
Bioactivity


英文名: Omecamtiv mecarbil

描述: Omecamtiv mecarbil (CK-1827452) 是一种心脏特异性的肌球蛋白激活剂，用于研究心脏相关疾病。

激酶实验: Axl Kinase activity assay: Test compounds are diluted to desired concentrations in kinase reaction buffer (50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM EGTA, 2 mM DTT, and 0.01% v/v Tween-20) and are briefly incubated with Axl kinase. The Axl kinase used is recombinant human Axl kinase (catalytic domain, amino acids 473-894) with a histidine tag. The reaction is initiated by the addition of ATP and fluorescein-labeled poly-GT substrate (poly Glu:Tyr, 4:1 polymer). Concentration of the various components in the assay (10 μL reaction volume) are: 1% DMSO, 93 ng/mL Axl kinase, 20 μM ATP, and 200 nM fluorescein poly-GT substrate. Following addition of ATP and fluorescein poly-GT substrate, incubation is for 60 min at room temperature, the enzyme reaction is stopped by addition of 10 μL terbium-labeled anti-phosphotyrosine PY20 antibody in EDTA-containing buffer. Final concentration of EDTA and antibody after addition to the reaction is 10 mM and 2 nM, respectively. The terbium conjugated antibody generates a time-resolved FRET signal with the fluorescein molecule (bound to the poly-GT substrate) when the substrate is phosphorylated. After one hour incubation at room temperature, fluorescence is measured with excitation of 320 nm and dual emission of 495 and 520 nm on an EnVision microplate reader. Signal is expressed in -636996terms of a TR-FRET ratio (fluorescence intensity at 520 nm to 495 nm).

体外活性: Omecamtiv mecarbil会导致一些血流动力学参数（包括心率,平均左心房压力和左心室舒张末期压力）的下降.OOmecamtiv mecarbil在左心室肥大的清醒的狗体内,对血流动力学参数产生相似且无统计学差异的影响.在有心肌梗死（MI-sHF）的有意识的狗中,Omecamtiv mecarbil导致壁增厚（25％）,每搏输出量（44％）,心输出量（22％）和左心室（LV）收缩射血时间显著增加（26％）.

体内活性: 在离体心肌细胞中,Omecamtiv mecarbil可以增加肌细胞收缩力,克服肌球蛋白抑制剂BDM而不增加钙瞬变或抑制PDE通路。在体外,Omecamtiv mecarbil通过增加肌球蛋白ATPase速率选择性地激活心肌肌球蛋白。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 6 mg/mL (14.94 mM)
DMSO : 74 mg/mL (184.3 mM)


关键字: CK1827452 | Inhibitor | inhibit | CK 1827452 | Myosin | Omecamtiv mecarbil

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途