TRANS-1-(4-HYDROXYCYCLOHEXYL)-4-(4-FLUOROPHENYL)-5-(2-METHOXYPYRIMIDIN-4-YL) IMIDAZOLE
SB 239063
CAS: 193551-21-2
Molecular Formula: C20H21FN4O2
TRANS-1-(4-HYDROXYCYCLOHEXYL)-4-(4-FLUOROPHENYL)-5-(2-METHOXYPYRIMIDIN-4-YL) IMIDAZOLE - Names and Identifiers
TRANS-1-(4-HYDROXYCYCLOHEXYL)-4-(4-FLUOROPHENYL)-5-(2-METHOXYPYRIMIDIN-4-YL) IMIDAZOLE - Physico-chemical Properties
| Molecular Formula | C20H21FN4O2 |
| Molar Mass | 368.4 |
| Melting Point | 206-207.2°C |
| Solubility | DMSO: 11mg/mL |
| Appearance | White solid |
| Color | white |
| Storage Condition | 2-8°C |
| In vitro study | 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. |
| In vivo study | 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. |
TRANS-1-(4-HYDROXYCYCLOHEXYL)-4-(4-FLUOROPHENYL)-5-(2-METHOXYPYRIMIDIN-4-YL) IMIDAZOLE - Risk and Safety
| Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 3 |
| RTECS | GV9458000 |
TRANS-1-(4-HYDROXYCYCLOHEXYL)-4-(4-FLUOROPHENYL)-5-(2-METHOXYPYRIMIDIN-4-YL) IMIDAZOLE - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.714 ml | 13.572 ml | 27.144 ml |
| 5 mM | 0.543 ml | 2.714 ml | 5.429 ml |
| 10 mM | 0.271 ml | 1.357 ml | 2.714 ml |
| 5 mM | 0.054 ml | 0.271 ml | 0.543 ml |
Last Update：2024-01-02 23:10:35
TRANS-1-(4-HYDROXYCYCLOHEXYL)-4-(4-FLUOROPHENYL)-5-(2-METHOXYPYRIMIDIN-4-YL) IMIDAZOLE - Reference Information
| biological activity | SB239063 is an effective selective p38 MAPK α/β inhibitor with IC50 of 44 nM and no activity against γ-and δ-kinase subtypes. |
| target | TargetValue p38α (cell-free say) 44 nM p38β (cell-free say) 44 nM |
| Target | Value |
| p38α (Cell-free assay) | 44 nM |
| p38β (Cell-free assay) | 44 nM |
| in vitro study | 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 Concentration: 0.1 μM, 1 μM, 10 μM 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. |
| 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. Significantly inhibited the resultant antigen-induced airport eosinophilia. |
| in vivo study | 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 airport eosinophilia. SB 239063 (12 mg/kg; P. o.) almost abolishes ovalbumin (OA)-induced airport eosinophilia (~ 93% inhibition) by inhalation. SB 239063 is a potent inhibitor of LPS-induced TNF-alpha production in the mouse peritoneal capacity with an EC 50 of 5.8 mg/kg (2.8-10.3; 95% CL). Animal Model: Male BALB/C MICE (18-20g) 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. |
| 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 |
Last Update：2024-04-10 22:29:15
Supplier List
Spot supply
Product Name: SB 239063 Visit Supplier Webpage Request for quotationCAS: 193551-21-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Spot supply
Product Name: SB 239063 Visit Supplier Webpage Request for quotationCAS: 193551-21-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History