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. |
Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
WGK Germany | 3 |
RTECS | GV9458000 |
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 |
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 |