货号	规格	价格	上海	北京	珠海	重庆	武汉
S81048-1mg买3赠1	99.40%	￥80.00 S81048-1mg ￥80.00 现货（买3赠1）	6 6	-	-	-	-
S81048-2mg买3赠1	99.40%	￥99.00 S81048-2mg ￥99.00 现货（买3赠1）	6 6	-	-	-	-
S81048-5mg	99.40%	￥126.00 S81048-5mg ￥126.00 现货	7 7	-	-	-	-
S81048-10mg	99.40%	￥238.00 S81048-10mg ￥238.00 现货	7 7	-	-	-	-
S81048-25mg	99.40%	￥490.00 S81048-25mg ￥490.00 现货	3 3	-	-	-	-
S81048-50mg	≥99%	￥700.00 S81048-50mg ￥700.00 2-3天	0 货期：2-3天	-	-	-	-
S81048-100mg	≥99%	￥1350.00 S81048-100mg ￥1350.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

Omecamtiv mecarbil (CK-1827452) is a selective cardiac myosin activator.

靶点：

Myosin;ATPase; Myosin

体内研究：

Omecamtiv mecarbil (100-1000 ng/mL) demonstrates concentration-dependent increases in FS in Sprague−Dawley rats model. Omecamtiv mecarbil demonstrates good PK parameters in both rats (Sprague−Dawley) and dogs (Beagle) with clearances of 22 and 7.2 mL/min/kg, volumes of 3.5 and 3.6 L/kg, and bioavailabilities (F%) of 100 and 80%, respectively. Omecamtiv mecarbil does not affect the phosphorylation status of myofilament proteins in both WT and KO hearts as shown by the absence of significant differences between pre and post Omecamtiv mecarbil samples within WT and KO groups, or affect the force generation at maximal Ca2+ activation (pCa 4.5) in any of the groups. Omecamtiv mecarbil increases the responsiveness of the cardiac myofilaments to Ca2+ at submaximal Ca2+-activations.

参考文献：

1. Morgan BP, et al. Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac Myosin. ACS Med Chem Lett. 2010 Aug 20;1(9):472-7. 2. Mamidi R, et al. Molecular effects of the myosin activator omecamtiv mecarbil on contractile properties of skinned myocardium lacking cardiac myosin binding protein-C. J Mol Cell Cardiol. 2015 Aug;85:262-72. 3. Swenson AM, et al. Omecamtiv Mecarbil Enhances the Duty Ratio of Human β-Cardiac Myosin Resulting in Increased Calcium Sensitivity and Slowed Force Development in Cardiac Muscle. J Biol Chem. 2017 Mar 3;292(9):3768-3778.

溶解性：

DMSO : 20 mg/mL (49.82 mM; ultrasonic and warming and heat to 60°C)

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.491 ml	12.455 ml	24.911 ml
5 mM	0.498 ml	2.491 ml	4.982 ml
10 mM	0.249 ml	1.246 ml	2.491 ml
50 mM	0.05 ml	0.249 ml	0.498 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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