KN-92 phosphate
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KN-92是Ca2+/钙调素依赖性激酶II（CaMKII）抑制剂KN-93的无活性类似物。KN-92常被用作KN-93的阴性对照。KN-92显著降低Kv通道的5-s去极化脉冲结束时的持续电流振幅，如Kv1.5和Kv1.2 [1]。
参考文献：
Rezazadeh S, Claydon TW, Fedida D. KN-93(2-[N-(2-hydroxyethyl)]-N-(4-methoxybenzenesulfonyl)]amino-N-(4-chlorocinnamyl)-N-methylbenzylamine), a calcium/calmodulin-dependent protein kinase II inhibitor, is a direct extracellular blocker of voltage-gated potassium channels. J Pharmacol Exp Ther. 2006 Apr;317(1):292-9.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 554.98 |
| Cas No. | 1135280-28-2 |
| Formula | C24H28ClN2O7PS |
| Synonyms | KN 92 phosphate;KN92 phosphate |
| Solubility | ≥25 mg/mL in DMSO; insoluble in H2O; ≥43.1 mg/mL in EtOH with gentle warming |
| Chemical Name | (E)-N-(2-(((3-(4-chlorophenyl)allyl)(methyl)amino)methyl)phenyl)-4-methoxybenzenesulfonamide phosphate |
| SDF | Download SDF |
| Canonical SMILES | CN(CC1=CC=CC=C1NS(C2=CC=C(OC)C=C2)(=O)=O)C/C([H])=C([H])/C3=CC=C(Cl)C=C3.OP(O)(O)=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]: | |
|
细胞系 |
兔肥大心肌细胞 |
|
溶解方法 |
该化合物在DMSO中的溶解度>25mg/mL。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
|
反应条件 |
0.5 μmol/L和1 μmol/L |
|
应用 |
KN-92是KN-93的无活性类似物。在低钾，低镁Tyrode溶液灌注和慢频电刺激的条件下，假手术组、左心室肥大（LVH）组、KN-92组（0.5μmol/ L）和KN-93组（0.5μmol/ L）早期去极化（EAD）的发生率分别为0/12，11/12，10/12和5/12。KN-92组和KN-93组药物浓度增加至1μmol/ L时，EAD的发生率分别为10/12和2/12。当KN-92和KN-93组药物浓度为0.5μmol/ L时，0 mV时的峰值ICa，L分别降低了（9.4±2.8）％和（10.5±3.0）％。当药物浓度增加到1μmol/ L时，峰值ICa，L值分别降低了（13.4±3.7）％和（40±4.9）％。 |
| 动物实验[2]: | |
|
动物模型 |
自发性高血压大鼠 |
|
剂量 |
1 μmol/L |
|
应用 |
在自发性高血压大鼠中，动作电位持续时间交替（APD-ALT）在显著更低的起搏速率下诱发，KN-93（1μmol/ L），而不是其无活性类似物KN-92（1μmol/ L）完全逆转APD-ALT的这些变化。APD-ALT的幅度在SHR中显著高于WKY大鼠，并且可被KN-93完全正常化。KN-93也消除了SHR中快速起搏引起的心室颤动（VF）。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同，这是由实验系统的误差引起的，属于正常现象。 |
|
References: [1]. Ke J1, Chen F, Zhang C, et al. Effects of calmodulin-dependent protein kinase II inhibitor, KN-93, on electrophysiological features of rabbit hypertrophic cardiac myocytes. J Huazhong Univ Sci Technolog Med Sci. 2012 Aug;32(4):485-9. [2]. Mitsuyama H1, Yokoshiki H2, Watanabe M1, et al. Ca2+/calmodulin-dependent protein kinase II increases the susceptibility to the arrhythmogenic action potential alternans in spontaneously hypertensive rats. Am J Physiol Heart Circ Physiol. 2014 Jul 15;307(2):H199-206. |
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质量控制和MSDS
- 批次:
化学结构
