切换导航

SB 239063

现货
Catalog No.
A3792
p38 MAP激酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,210.00
现货
5mg
¥ 990.00
现货
25mg
¥ 3,490.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

SB239063 is a potent and selective p38 MAPK inhibitor with an IC50 of 44 nM against p38α MAPK while exihibited no activity against the γ- and δ-kinase isoforms [1].

In vitro: In oxygen-glucose-deprived hippocampal slice cultures, treatment with 20 μM and 100 μM SB239063 significantly reduced the levels of the pro-inflammatory cytokine IL-1β and reduced cell death after oxygen-glucose deprivation and strikingly diminished microglia activation[2].

In vivo: Oral administration of 3–30 mg/kg SB 239063 given twice a day dose-dependently inhibited airway neutrophil infiltration and interleukin (IL)-6 levels 48 h after lipopolysaccharide (LPS) inhalation [1]. In a bleomycin-induced pulmonary fibrosis model rats, SB 239063 treatment (2.4 or 4.8 mg/day via osmotic pump) significantly inhibited bleomycin-induced right ventricular hypertrophy (indicative of secondary pulmonary hypertension) and increased in lung hydroxyproline synthesis (indicative of collagen synthesis and fibrosis) (1). In conscious guinea pigs, administration of SB 239063 (10 or 30 mg/kg p.o.) showed approximately 50% inhibition of OA-induced pulmonary eosinophil influx, measured by BAL 24 h after antigen(1). Orally administration of SB 239063 (30 mg/kg) attenuated IL-6 bronchoalveolar lavage fluid concentrations (> 90% inhibition) and MMP-9 activity (64% inhibition) measured 6 h after LPS exposure. In guinea pig cultured alveolar macrophages, SB 239063 inhibited LPS-induced IL-6 production with IC50 of 362 nM. In lipopolysaccharide-stimulated human peripheral blood monocytes, SB 239063 inhibited IL-1 and TNF-α production with an IC50 of 0.12 and 0.35 μM, respectively(1).

References:
[1] Underwood D C, Osborn R R, Bochnowicz S, et al.  SB 239063, a p38 MAPK inhibitor, reduces neutrophilia, inflammatory cytokines, MMP-9, and fibrosis in lung[J]. American Journal of Physiology-Lung Cellular and Molecular Physiology, 2000, 279(5): L895-L902.
[2] Strassburger M, Braun H, Reymann K G.  Anti-inflammatory treatment with the p38 mitogen-activated protein kinase inhibitor SB239063 is neuroprotective, decreases the number of activated microglia and facilitates neurogenesis in oxygen–glucose-deprived hippocampal slice cultures[J]. European journal of pharmacology, 2008, 592(1): 55-61.

文献引用

1. MXinwei Feng1, Junfeng Lu2, et al. "Mycobacterium smegmatis Induces Neurite Outgrowth and Differentiation in an Autophagy-Independent Manner in PC12 and C17.2 Cells." Front. Cell. Infect. Microbiol., 19 June 2018.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt368.4
Cas No.193551-21-2
FormulaC20H21FN4O2
SynonymsSB-239063;SB239063
Solubility≥18.4 mg/mL in DMSO, ≥46.8 mg/mL in EtOH with ultrasonic and warming, <2.28 mg/mL in H2O
Chemical Name4-(4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl)cyclohexanol
SDFDownload SDF
Canonical SMILESCOC1=NC=CC(C2=C(C3=CC=C(F)C=C3)N=CN2C4CCC(O)CC4)=N1
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

人离体全血

制备方法

在DMSO中的溶解度大于18.4 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

0.01 ~ 10 μM;4小时

实验结果

在脂多糖刺激的人全血中,SB 239063浓度依赖性地抑制一系列炎性细胞因子(包括IL-1、TNF-α、IL-8和IL-6)合成,其IC50值为0.02 ~ 0.09 μM。相比,SB 239063对IL-1ra仅有较弱的抑制作用,其IC50值约为2 μM。

动物实验 [1]:

动物模型

Bleomycin诱导的肺纤维化大鼠模型

给药剂量

2.4或4.8 mg/day;通过渗透泵给药

实验结果

在Bleomycin诱导的肺纤维化大鼠模型中,SB 239063显著抑制Bleomycin诱导的右心室肥大(指示继发性肺动脉高压),同时显著减少Bleomycin诱导的肺羟脯氨酸合成(指示胶原合成和纤维化)。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Underwood D C, Osborn R R, Bochnowicz S, et al. SB 239063, a p38 MAPK inhibitor, reduces neutrophilia, inflammatory cytokines, MMP-9, and fibrosis in lung[J]. American Journal of Physiology-Lung Cellular and Molecular Physiology, 2000, 279(5): L895-L902.

质量控制

化学结构

MLN9708

相关生物数据

MLN9708