|(S)-4-(2-(N-甲基异喹啉-5-磺胺)-3-氧代-3-(4-苯基哌嗪-1-基)丙基)苯基异喹啉-5-磺酸盐|CsnPharm

CAS No.: 127191-97-3

KN-62 Catalog No. CSN11254

Synonyms: KN-62

KN-62 is a selective and potent inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with IC50 of 0.9 μM, KN-62 also displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM..

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述KN-62 is a multiple target as a selective and non-competitive P2X7 antagonist with IC50 value of 15-100nM for antagonizing the human P2X7 receptor and a CaMKII inhibitor with Ki value of 0.9μM for inhibition of phosphorylation of exogenous substrate (chicken gizzard myosin 20-kDa light chain). KN-62 could inhibit the Ca²⁺/calmodulin- dependent autophosphorylation of both α and β subunits of Ca2+/CaM kinase II dose-dependently in the presence or absence of exogenous substrate, without inhibition on autophosphorylated Ca2+/CaM kinase II. KN-62 at concentration of 0.5μM suppressed autophosphorylation of the 53-kDa subunit of Ca²⁺/CaM kinase in PC12 D cells. KN-62 strongly suppressed the CA1 region LTP at 3μM in rat hippocampal slices when applied prior to, not immediately after, a tetanic stimulation.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HEK293 cells	-	Function assay	-	Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium influx, IC50=50.12 nM	19191585
human lymphocytes	-	Function assay	-	Antagonist activity at P2X7 receptor in human lymphocytes assessed as inhibition of ATP-induced Ba2+ influx, IC50=12.59 nM	19191585
THP1 cells	-	Function assay	-	Inhibition of Bz-ATP-induced IL1-beta release in LPS/IFN-gamma-differentiated human THP1 cells by ELISA, IC50=0.081 μM	19110420

动物研究
剂量
Nude Mice: 5 mg/kg^[3] (i.p.) Rat: 10 mg/kg^[4] (i.v.)

给药途径
i.p., i.v.
参考文献

动物研究
剂量	Nude Mice: 5 mg/kg^[3] (i.p.) Rat: 10 mg/kg^[4] (i.v.)
给药途径	i.p., i.v.

[1] Manosso LM, Moretti M, et al. Antidepressant-like effect of zinc is dependent on signaling pathways implicated in BDNF modulation. Prog Neuropsychopharmacol Biol Psychiatry. 2015 Jun 3;59:59-67.
[2] Ravi RG, Kertesy SB, et al. Potent P2X(7) Receptor Antagonists: Tyrosyl Derivatives Synthesized Using a Sequential Parallel Synthetic Approach. Drug Dev Res. 2001 Oct;54(2):75-87.

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
- 1.3853 mL
- 6.9267 mL
- 13.8535 mL
- 5 mM
- 0.2771 mL
- 1.3853 mL
- 2.7707 mL
- 10 mM
- 0.1385 mL
- 0.6927 mL
- 1.3853 mL

技术信息

CAS号

127191-97-3

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C38H35N5O6S2

运输

蓝冰

分子量

721.84

别名

KN-62

溶解度

DMSO	480.0 mg/mL (665.0 mM)
Water	insoluble

动物实验配方

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KN-62 Catalog No. CSN11254

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