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1-[2-(4-甲氧基)-2-[3-(4-甲氧基苯基)丙氧基]乙基]咪唑

用途

SKF-96365 hydrochloride 是非选择性的TRP通道抑制剂。

名称

[ CAS 号 ]:
130495-35-1

[ 中文名 ]:
1-[β-(3-(4-甲氧基苯基)丙氧基)-4-甲氧苯]-1H-咪唑盐酸盐

[ 英文名 ]:
SKF-96365

[中文别名 ]:

[英文别名 ]:

UNII:33BI32858P
MFCD00236407
SKF 96365
SKF-96365 hydrochloride
SKF 96365 HCI

生物活性

[ 描述 ]:

SKF-96365 hydrochloride 是非选择性的TRP通道抑制剂。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

信号通路 >> 跨膜转运 >> TRP频道

研究领域 >> 癌症

[ 靶点 ]

TRP Channel[1]

[体外研究]

SKF-96365通过在结肠直肠癌细胞中诱导细胞周期停滞和凋亡而表现出有效的抗肿瘤活性。 SKF-96365以浓度依赖性方式抑制hERG电流[1]。 SKF-96365可通过阻止细胞色素c(cyt c)从线粒体释放到细胞质中而诱导细胞保护性自噬以延迟细胞凋亡。机械地,SKF-96365处理抑制钙/钙调蛋白依赖性蛋白激酶IIγ(CaMKIIγ)/ AKT信号级联。 CaMKIIγ或AKT的过度表达消除了SKF-96365对癌细胞的作用,表明CaMKIIγ/ AKT信号通路在SFK-96365诱导的生物学效应中起关键作用[2]。

[体内研究]

SKF-96365抑制体内CRC细胞生长。 SKF-96365处理导致小鼠中p-CaMKII和p-AKT的减少以及LC3-II,切割的PARP,caspase-3和caspase-9的增加[2]。

[动物实验]

小鼠：将5至6周龄雌性无胸腺BALB / c小鼠用HCT116细胞接种到右侧oxter中。当皮下肿瘤的直径达到约0.5cm时，将动物随机分配给载体，单独使用SKF-96365，单独使用HCQ或使用SKF-96365 + HCQ。施用SKF-96365（20mg / kg）并通过ip注射每天施用HCQ（60mg / kg）连续14天。确定肿瘤大小和体积。每组包括8只小鼠。在最后一次处理后24小时处死小鼠。将肿瘤称重并加工用于蛋白质印迹分析或石蜡包埋[2]。

[参考文献]

[1]. Liu H, et al. SKF-96365 blocks human ether-à-go-go-related gene potassium channels stably expressed in HEK 293 cells. Pharmacological Research. Pharmacol Res, 2016 Feb, 104:61-9.

[2]. Jing Z, et al. SKF-96365 activates cytoprotective autophagy to delay apoptosis in colorectal cancer cells through inhibition of the calcium/CaMKIIγ/AKT-mediated pathway. Cancer Lett, 2016 Mar 28, 372(2):226-38.

[相关活性小分子]

辣椒碱 | 辣椒平 | 5-(N-乙基-N-异丙基)阿米洛利 | 氯化二亚苯基碘鎓 | 2-(1,3-二甲基-2,6-二氧代-2,3-二氢-1H-嘌呤-7(6H)-基)-N-(4-异丙基苯基)乙酰胺 | HC-067047 | AMG9810 | GSK1016790A | SAR7334 | PF-4840154 | RN-1734 | AMG 517 | 3-(4-氯苯基)-N-(3-甲氧基苯基)-2-丙烯酰胺 | 冰素 | ML204

物理化学性质

[ 沸点 ]:
556ºC at 760mmHg

[ 熔点 ]:
119 °C

[ 分子式 ]:
C₂₂H₂₇ClN₂O₃

[ 分子量 ]:
402.914

[ 闪点 ]:
290.1ºC

[ 精确质量 ]:
402.171021

[ PSA ]:
45.51000

[ LogP ]:
5.09300

[ 外观性状 ]:
solid | white

[ 蒸汽压 ]:
7.86E-12mmHg at 25°C

[ 储存条件 ]:
Store at RT

[ 水溶解性 ]:
H2O: >20 mg/mL

MSDS

详细MSDS(安全技术说明书)

安全信息

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

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36

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

[ WGK德国 ]:
3

[ 海关编码 ]:
2933290090

海关

[ 海关编码 ]: 2933290090

[ 中文概述 ]:
2933290090. 其他结构含非稠合咪唑环的化合物. 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 ]:
2933290090. other compounds containing an unfused imidazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

文献

Mechanosensitive Ca²⁺-permeable channels in human leukemic cells: pharmacological and molecular evidence for TRPV2.

Biochim. Biophys. Acta 1848(1 Pt A) , 51-9, (2015)

Mechanosensitive channels are present in almost every living cell, yet the evidence for their functional presence in T lymphocytes is absent. In this study, by means of the patch-clamp technique in at...

STIM1 phosphorylation triggered by epidermal growth factor mediates cell migration.

Biochim. Biophys. Acta 1853(1) , 233-43, (2015)

STIM1 is a key regulator of store-operated calcium entry (SOCE), and therefore a mediator of Ca²⁺ entry-dependent cellular events. Phosphorylation of STIM1 at ERK1/2 target sites has been described as...

ATP releases ATP or other nucleotides from human peripheral blood leukocytes through purinergic P2 receptors.

Life Sci. 145 , 85-92, (2016)

Almost every eukaryotic cell releases ATP under certain conditions. The idea that ATP induces the release of ATP has been scantly investigated.We explored this possibility by assessing the rate of exo...

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