4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶 CAS#: 193746-75-7

4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶

生物活性靶点体外研究体内研究用途与合成方法 MSDS 4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶价格(试剂级) 上下游产品信息

中文名称	4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶
中文同义词	4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶;P38MAP激酶抑制剂(SB 242235);化合物SB242235;4-(4-(4-氟苯基)-1-(哌啶-4-基)-1H-咪唑-5-基)-2-甲氧基嘧啶
英文名称	SB242235
英文同义词	SB242235;4-[4-(4-Fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-2-methoxypyrimidine;4-(4-(4-Fluorophenyl)-1-(piperidin-4-yl)-1H-iMidazol-5-yl)-2-MethoxypyriMidine;SB-242235; SB242235;CS-668;SB242235 ≥95%;Pyrimidine, 4-[4-(4-fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-2-methoxy-;inhibit,SB 242235,Autophagy,Inhibitor,p38 MAPK
CAS号	193746-75-7
分子式	C19H20FN5O
分子量	353.39
EINECS号
相关类别	细胞生物学试剂
Mol文件	193746-75-7.mol
结构式

4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶性质

沸点	568.4±60.0 °C(Predicted)
密度	1.34
储存条件	2-8°C(protect from light)
溶解度	DMF：25mg/mL； DMSO：20mg/mL；乙醇：30mg/mL
形态	粉末
酸度系数(pKa)	9.91±0.10(Predicted)

4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶用途与合成方法

生物活性

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。

靶点

IC50: 1.0　μM (p38 MAPK, primary human chondrocytes)

体外研究

SB 242235 (0-10　μM) dose-dependently inhibits the activation of MAPKAP K2 with an IC ₅₀ 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.

Western Blot Analysis

Cell Line:	Human chondrocytes
Concentration:	0 μM,0.01 μM,0.1 μM,1 μM,10　μM
Incubation Time:	15 minutes
Result:	Dose-dependently inhibited the activation of MAPKAP K2 with an IC ₅₀ of 1.0 μM.

体内研究

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.

Animal Model:	Female SKH-1 hairless mice (4–6 weeks)
Dosage:	100 mg/kg
Administration:	Oral administered, 30 minutes prior to ultraviolet B (UVB) irradiation
Result:	Abolished MAP-KAPK-2 activity and heat shock protein 27 (HSP27) phosphorylation.

安全信息

海关编码	2924297099

MSDS信息

4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶价格(试剂级)

更新日期	产品编号	产品名称	CAS号	包装	价格
2024/04/30	HY-18306	4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶 SB 242235	193746-75-7	5mg	850元
2024/04/30	HY-18306	4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶 SB 242235	193746-75-7	10mM * 1mLin DMSO	935元

4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶