|(E)-N-(2-(((3-(4-氯苯基)烯丙基)(甲基)氨基)甲基)苯基)-N-(2-羟乙基)-4-甲氧基苯磺酰胺磷酸盐|CsnPharm

CAS No.: 1188890-41-6

KN-93 磷酸盐 Catalog No. CSN18794

Synonyms: KN-93;KN-93 phosphate

KN-93 Phosphate, a potent Ca2+/calmodulin-dependent protein kinase II (CaMKII) selective inhibitor with Ki of 370 nM, is the water soluble version of KN-93.

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400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 CaMKII

Ki:0.37μM
描述KN-93 Phosphate is the phosphate form of KN-93. KN-93 is a CaMKII (Calcium/calmodulin-dependent protein kinase II) blocker. It elicited potent inhibitory effects on CaMKII phosphorylating activity with an inhibition constant of 0.37μM but had no significant effects on the catalytic activity of CAMP-dependent protein kinase, Ca²⁺/phospholipid dependent protein kinase, myosin light chain kinase and Ca²⁺-phosphodiesterase. KN-93 also inhibited the autophosphorylation of both the α- and β-subunits of CaMKII. KN-93 inhibited dopamine formation by modulating the reaction rate of TH to reduce the Ca²⁺-mediated phosphorylation levels of the tyrosine hydroxylase molecule in PC12h cells. KN-93 also works as a direct extracellular blocker of voltage-gated potassium channels with IC50 value of 307±12nM for block of the Kv1.5. KN-93 acted through promotion and stabilization of C-type inactivation. KN-93 was ineffective as a blocker when applied intracellularly, suggesting that CaMK II-independent effects of KN-93 on Kv channels can be circumvented by intracellular application of KN-93. KN-93 inhibits I_Kr in mammalian cardiomyocytes.
动物研究
剂量
Rat: 0.501 μg/kg^[3] (p.o.), 1 mg/kg^[4] (i.p.) Woodchucks: 125 μg/kg^[5] (osmotic minipumps) Mice: 4 mg/kg (i.p.)

给药途径
p.o., osmotic minipumps, i.p.

动物研究
剂量	Rat: 0.501 μg/kg^[3] (p.o.), 1 mg/kg^[4] (i.p.) Woodchucks: 125 μg/kg^[5] (osmotic minipumps) Mice: 4 mg/kg (i.p.)
给药途径	p.o., osmotic minipumps, i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.6694 mL
- 8.3468 mL
- 16.6936 mL
- 5 mM
- 0.3339 mL
- 1.6694 mL
- 3.3387 mL
- 10 mM
- 0.1669 mL
- 0.8347 mL
- 1.6694 mL

技术信息

CAS号

1188890-41-6

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H32ClN2O8PS

运输

蓝冰

分子量

599.03

别名

KN-93;KN-93 phosphate

溶解度

DMSO	80.0 mg/mL (133.5 mM) warming
Water	15.0 mg/mL (25.0 mM) warming

动物实验配方

0.5% CMC-Na

40 mg/mL

suspension

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KN-93 磷酸盐 Catalog No. CSN18794

靶点选择性

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