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N-环己基-N-[2-(3,5-二甲基吡唑-1-基)-6-甲基嘧啶-4-基]胺

用途

CyPPA 是 hSK3 和 hSK2 的阳性调节剂,其 EC50 值分别为 14 μM 和5.6 μM。CyPPA 对 hSK1 和 hIK 通道无活性。

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名称

[ CAS 号 ]:
73029-73-9

[ 中文名 ]:
N-环己基-N-[2-(3,5-二甲基吡唑-1-基)-6-甲基嘧啶-4-基]胺

[ 英文名 ]:
CyPPA

[中文别名 ]:

[英文别名 ]:

Synthalin sulfate
CyPPA

生物活性

[ 描述 ]:

CyPPA 是 hSK3 和 hSK2 的阳性调节剂,其 EC50 值分别为 14 μM 和5.6 μM。CyPPA 对 hSK1 和 hIK 通道无活性。

[ 相关类别 ]:

研究领域 >> 神经疾病

信号通路 >> 跨膜转运 >> 钾通道

[体外研究]

cypa诱导通道激活的表观Ca2+敏感性增加,使EC50(Ca2+)从429nm变为59nm[1]。

[体内研究]

CyPPA是一种小电导钙激活K+通道的阳性调节剂,它能抑制小鼠的子宫收缩并延缓早产[2]。

[参考文献]

[1]. Neurons, Inhibits Dopamine Release, and Counteracts Hyperdopaminergic Behaviors Induced by Methylphenidate. Br J Pharmacol. 2007 Jul;151(5):655-65.

[2]. Dana V Skarra, et al. CyPPA, a positive modulator of small-conductance Ca(2+)-activated K(+) channels, inhibits phasic uterine contractions and delays preterm birth in mice. Am J Physiol Cell Physiol. 2011 Nov;301(5):C1027-35.

物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
512.2±42.0 °C at 760 mmHg

[ 分子式 ]:
C₁₆H₂₃N₅

[ 分子量 ]:
285.387

[ 闪点 ]:
263.6±27.9 °C

[ 精确质量 ]:
285.195343

[ PSA ]:
55.63000

[ LogP ]:
2.13

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.648

[ 储存条件 ]:
2-8℃

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335-H413

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
36/37/38

[ 安全声明 (欧洲) ]:
26-36/37

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2933990090

海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

文献

Duration differences of corticostriatal responses in striatal projection neurons depend on calcium activated potassium currents.

Front. Syst. Neurosci. 7 , 63, (2013)

The firing of striatal projection neurons (SPNs) exhibits afterhyperpolarizing potentials (AHPs) that determine discharge frequency. They are in part generated by Ca(2+)-activated K(+)-currents involv...

Identification of the functional binding pocket for compounds targeting small-conductance Ca²⁺-activated potassium channels.

Nat. Commun. 3 , 1021, (2012)

Small- and intermediate-conductance Ca(2+)-activated potassium channels, activated by Ca(2+)-bound calmodulin, have an important role in regulating membrane excitability. These channels are also linke...

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