Rimacalib (Synonyms: SMP 114)
目录号: PL01130 纯度: ≥99%
CAS No. :215174-50-8
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中文名称
Rimacalib
英文名称
Rimacalib
英文别名
4-Morpholinecarboximidamide,N-[3-[(1S)-1-(2-fluoro[1,1'-biphenyl]-4-yl)ethyl]-5-isoxazolyl]-;N'-[3-[(1S)-1-(3-fluoro-4-phenylphenyl)ethyl]-1,2-oxazol-5-yl]morpholine-4-carboximidamide;Rimacalib;SMP 114;BZ76J3N815;Rimacalib [INN];DB12571;N'-(3-((1S)-1-(2-fluoro-4-biphenylyl)ethyl)-1,2-oxazol-5-yl)-4-morpholinecarboximidamide;N-(3-((1S)-1-(2-Fluorobiphenyl-4-yl)ethyl)-1,2-oxazol-5-yl)morpholine-4-carboximidamide;4-Morpholinecarboximidamide, N-(3-((1S)-1-(2-fluoro(1,1'-biphenyl)-4-yl)ethyl)-5-isoxazolyl)-
Cas No.
215174-50-8
分子式
C22H23FN4O2
分子量
394.44
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
Rimacalib (SMP 114) 是一种 CaMKII 的抑制剂,其对 CaMKII 亚型的 IC50 值为 1-30 μM。
生物活性
Rimacalib (SMP 114) is a Ca/calmodulin-dependent protein kinase II (CaMKII) inhibitor, with IC 50 s of ~1 μM for CaMKIIα to ~30 μM for CaMKIIγ.
性状
Solid
IC50 & Target[1][2]
CaMK IIα 1 μM (IC50) CaMK IIγ 30 μM (IC
体外研究(In Vitro)
Rimacalib (SMP-114) improves (by ~40%) Ca-transient potentiation during the 30 s stimulation pause, higher Fura-2 transient amplitude after the pause upon Rimacalib vs. 37.2±4.3% in control, n=60/17 cells/mice vs. n=65/17, p<0.05) and in parallel cardiomyocyte contractility (135.0±15.4% vs. 97.2±16% increase of twitch amplitude, p=0.098). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
ClinicalTrial
参考文献
[1]. Neef S, et al. Reduction of SR Ca2+ leak and arrhythmogenic cellular correlates by SMP-114, a novel CaMKII inhibitor with oral bioavailability. Basic Res Cardiol. 2017 Jul;112(4):45.
溶解度数据
In Vitro: DMSO : 125 mg/mL (316.90 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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