4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶
- CAS号:193746-75-7
- 英文名:SB242235
- 中文名:4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶
- CBNumber:CB12621150
- 分子式:C19H20FN5O
- 分子量:353.39
- MOL File:193746-75-7.mol
- 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: 25 mg/ml; DMSO: 20 mg/ml; Ethanol: 30 mg/ml
- 形态 :Powder
- 酸度系数(pKa) :9.91±0.10(Predicted)
- 颜色 :White to off-white
- 海关编码 :2924297099
4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶性质、用途与生产工艺
- 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。
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靶点
IC50: 1.0 μM (p38 MAPK, primary human chondrocytes)
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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.
- 更新日期:2024/11/08
- 产品编号:HY-18306
- 产品名称:4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶 SB 242235
- CAS编号:193746-75-7
- 包装:5mg
- 价格:850元
- 更新日期:2024/11/08
- 产品编号:HY-18306
- 产品名称:4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶 SB 242235
- CAS编号:193746-75-7
- 包装:10mM * 1mLin DMSO
- 价格:935元
- 公司名称:CHEMSWORTH
- 联系电话:--
- 电子邮件:info@chemsworth.com
- 国家:印度
- 产品数:6700
- 优势度:30
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