反式-1-(4-羟基环己基)-4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)咪唑
- CAS号:193551-21-2
- 英文名:SB 239063
- 中文名:反式-1-(4-羟基环己基)-4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)咪唑
- CBNumber:CB6100319
- 分子式:C20H21FN4O2
- 分子量:368.4
- MOL File:193551-21-2.mol
- 熔点 :206-207.2 °C
- 储存条件 :2-8°C
- 溶解度 :DMSO: 11 mg/mL
- 形态 :White solid
- 颜色 :white
- InChIKey :ZQUSFAUAYSEREK-WKILWMFISA-N
- 安全说明 :22-24/25
- WGK Germany :3
- RTECS号 :GV9458000
- 海关编码 :2933599590
反式-1-(4-羟基环己基)-4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)咪唑性质、用途与生产工艺
- 生物活性 SB239063是一种有效的选择性p38 MAPKα/β抑制剂，IC50为44 nM，对γ- 和 δ-激酶亚型没有活性。
-
靶点
Target Value p38α
(Cell-free assay)44 nM p38β
(Cell-free assay)44 nM -
体外研究
SB 239063 (0.1–10 μM ; 29 hours, 47 hours) increases apoptosis of eosinophils in a dose-related in the presence of 10 pM IL-5 at every time point from 21 hours onwards.
SB 239063 potently inhibits IL-1 and TNF- a production in LPS-stimulated human peripheral blood monocytes with IC 50 values of 120 nM and 350 nM, respectively.
Apoptosis Analysis
Cell Line: Eosinophils (guinea pig BALs) Concentration: 0.1μM, 1μM, 10μM Incubation Time: 29 hours, 47 hours Result: Increased apoptosis of eosinophils in a dose-related in the presence of 10 pM IL-5 at every time point from 21 hours onwards. -
体内研究
SB 239063 (12 mg/kg; p.o.; 1 hour before and 4 hours after OA challenge; b.i.d. for 3 days) significantly inhibits the resultant antigen-induced airway eosinophilia.
SB 239063 (12 mg/kg; p.o.) almost abolishes ovalbumin (OA)-induced airway eosinophilia (~ 93% inhibition) by inhalation.
SB 239063 is a potent inhibitor of LPS-induced TNF-alpha production in the mouse peritoneal cavity with an EC 50 of 5.8 mg/kg (2.8–10.3; 95% CL).
Animal Model: Male BALB/c mice (18–20 g) Dosage: 12 mg/kg Administration: Oral administration; 1 h before and 4 h after OA challenge; bis in die for 3 days Result: Significantly inhibited the resultant antigen-induced airway eosinophilia.
- 更新日期：2024/11/08
- 产品编号：HY-11068
- 产品名称：反式-1-(4-羟基环己基)-4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)咪唑 SB 239063
- CAS编号：193551-21-2
- 包装：1mg
- 价格：500元
- 更新日期：2024/11/08
- 产品编号：HY-11068
- 产品名称：反式-1-(4-羟基环己基)-4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)咪唑 SB 239063
- CAS编号：193551-21-2
- 包装：10mM * 1mLin DMSO
- 价格：892元
- 公司名称：Carbosynth
- 联系电话：--
- 电子邮件：sales@carbosynth.com
- 国家：英国
- 产品数：6005
- 优势度：58
- 公司名称：TOCRIS-US
- 联系电话：--
- 电子邮件：customerservice@tocris.co.uk
- 国家：英国
- 产品数：5726
- 优势度：77
