SB 242235
目录号: PL08728 纯度: ≥99%
CAS No. :193746-75-7
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中文名称
SB 242235
中文别名
4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶;SB 242235
英文名称
SB 242235
英文别名
4-(4-(4-Fluorophenyl)-1-(piperidin-4-yl)-1H-imidazol-5-yl)-2-methoxypyrimidine;4-[5-(4-fluorophenyl)-3-piperidin-4-ylimidazol-4-yl]-2-methoxypyrimidine;SB 242235;SB-242235;4-[4-(4-Fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-2-methoxypyrimidine;SB242235;4-[4-(4-fluorophenyl)-1-(piperidin-4-yl)-1H-imidazol-5-yl]-2-methoxypyrimidine;Kinome_3169;BDBM15458;SYN1076;HMS3244I17;HMS3244I18;HMS3244J17;BCP05992;3254AH;AB0098302
Cas No.
193746-75-7
分子式
C19H20FN5O
分子量
353.39
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
SB-242235 是一种有效、选择性的 p38 MAP 激酶抑制剂,在人的软骨细胞中 IC50 值为 1.0 μM。
生物活性
SB-242235 is a potent and selective p38 MAP kinase inhibitor, with an IC 50 of 1.0 μM in primary human chondrocytes.
性状
Solid
IC50 & Target[1][2]
IC50: 1.0 μM (p38 MAPK, primary human chondrocytes)
体外研究(In Vitro)
SB 242235 (0-10 μM) dose-dependently inhibits the activation of MAPKAP K2 with an IC50 of 1.0 μM in human chondrocytes stimulated with IL-1β.
SB 242235 inhibits intracellular p38 activity, MAPKAP K2 was then isolated from these cells and assayed using HSP27 as a substrate.
has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis
体内研究(In Vivo)
SB242235 (100 mg/kg; p.o.) abolishes MAP-KAPK-2 activity and HSP27 phosphorylation.
SB242235 inhibits expression of the pro-inflammatory cytokines interleukin (IL)-6 and KC (murine IL-8) and COX-2.
SB-242235 is demonstrated non-linear elimination kinetics that manifested as a decrease in clearance with increasing dose and apparent oral bioavailability > 100% at high oral doses in rat and monkey.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Badger, A.M., et al., Differential effects of SB 242235, a selective p38 mitogen-activated protein kinase inhibitor, on IL-1 treated bovine and human cartilage/chondrocyte cultures. Osteoarthritis Cartilage, 2000. 8(6): p. 434-43.
[2]. Kim AL , et al. Role of p38 MAPK in UVB-induced inflammatory responses in the skin of SKH-1 hairless mice. J Invest Dermatol. 2005 Jun;124(6):1318-25.
溶解度数据
In Vitro: DMSO : ≥ 48 mg/mL (135.83 mM)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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