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6-(4-氟苯基)-5-(4-吡啶基)-2,3-二氢咪唑并[2,1-B]-噻唑

用途

SKF-86002是p38MAPK抑制剂,IC50值为0.5-1uM。

名称

[ CAS 号 ]:
72873-74-6

[ 中文名 ]:
6-(4-氟苯基)-5-(4-吡啶基)-2,3-二氢咪唑并[2,1-b]-噻唑

[ 英文名 ]:
SKF 86002

[英文别名 ]:

MFCD00869367
SKF-86002

生物活性

[ 描述 ]:

SKF-86002是p38MAPK抑制剂,IC50值为0.5-1uM。

[ 相关类别 ]:

信号通路 >> MAPK/ERK信号通路 >> p38 MAPK

研究领域 >> 炎症/免疫

[参考文献]

[1]. Griswold DE, et al. SK&F 86002: a structurally novel anti-inflammatory agent that inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid. Biochem Pharmacol. 1987 Oct 15;36(20):3463-70.

[2]. Frasch SC, et al. p38 mitogen-activated protein kinase-dependent and -independent intracellular signal transduction pathways leading to apoptosis in human neutrophils. J Biol Chem. 1998 Apr 3;273(14):8389-97.

[3]. Nick JA, et al. Common and distinct intracellular signaling pathways in human neutrophils utilized by platelet activating factor and FMLP. J Clin Invest. 1997 Mar 1;99(5):975-86.

[相关活性小分子]

物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
476.1±55.0 °C at 760 mmHg

[ 熔点 ]:
189-190ºC(lit.)

[ 分子式 ]:
C₁₆H₁₂FN₃S

[ 分子量 ]:
297.350

[ 闪点 ]:
241.7±31.5 °C

[ 精确质量 ]:
297.073608

[ PSA ]:
56.01000

[ LogP ]:
1.90

[ 蒸汽压 ]:
0.0±1.2 mmHg at 25°C

[ 折射率 ]:
1.713

[ 储存条件 ]:
2-8℃

安全信息

[ 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

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

[ 海关编码 ]:
2934100090

合成路线

详细合成路线

上下游产品

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海关

[ 海关编码 ]: 2934100090

[ 中文概述 ]:
2934100090. 结构上含有一个非稠合噻唑环的化合物(不论是否氢化). 增值税率:17.0%. 退税率:9.0%. 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

[ Summary ]:
2934100090 other compounds containing an unfused thiazole ring (whether or not hydrogenated) in the structure VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:20.0%

文献

The discovery of novel chemotypes of p38 kinase inhibitors.

Curr. Top. Med. Chem 5(10) , 953-65, (2005)

In the late 1970s and the early 1980s the initial p38 chemotype, the triaryl imidazoles, was discovered as an off-target effect during the development of cyclooxygenase and 5-lipoxygenase inhibitors l...

Activation of p38MAPK contributes to expanded polyglutamine-induced cytotoxicity.

PLoS ONE 3(5) , e2130, (2008)

The signaling pathways that may modulate the pathogenesis of diseases induced by expanded polyglutamine proteins are not well understood.Herein we demonstrate that expanded polyglutamine protein cytot...

Differential activation of the c-Jun N-terminal kinase pathway in arsenite-induced apoptosis and sensitization of chemically resistant compared to susceptible B-lymphoma cell lines.

Toxicol. Sci. 68(1) , 82-92, (2002)

Various forms of inorganic arsenic are significant environmental contaminants that have multiple effects on cells, including the induction of apoptotic cell death. Induction of apoptosis in lymphoid c...

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