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KN-92 phosphate

现货
Catalog No.
A3531
CaMKII抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 3,000.00
Ship with 10-15 days
5mg
¥ 2,460.00
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10mg
¥ 3,390.00
Ship with 10-15 days
50mg
¥ 9,860.00
Ship with 10-15 days
200mg
¥ 22,620.00
Ship with 10-15 days

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Background

KN-92 is the inactive analog of Ca2+/calmodulin-dependent kinase II (CaMKII) inhibitor KN-93. KN-92 has been often used as negative control for KN-93.KN-92 significantly reduced the sustained current amplitudes at the end of the 5-s depolarizing pulses of a wide range of Kv channels such as Kv1.5 and Kv1.2 [1].

Reference:
[1]. 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 PharmacolExpTher. 2006 Apr;317(1):292-9.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt554.98
Cas No.1135280-28-2
FormulaC24H28ClN2O7PS
SynonymsKN 92 phosphate;KN92 phosphate
Solubility≥25 mg/mL in DMSO, ≥43.1 mg/mL in EtOH with gentle warming, <1.54 mg/mL in H2O
Chemical Name(E)-N-(2-(((3-(4-chlorophenyl)allyl)(methyl)amino)methyl)phenyl)-4-methoxybenzenesulfonamide phosphate
SDFDownload SDF
Canonical SMILESCN(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
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议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。

试验操作

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.

质量控制

化学结构

KN-92 hydrochloride