Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C20H21FN4O2 |
| Molecular Weight | 368.4047 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=NC=CC(=N1)C2=C(N=CN2[C@H]3CC[C@H](O)CC3)C4=CC=C(F)C=C4
InChI
InChIKey=ZQUSFAUAYSEREK-WKILWMFISA-N
InChI=1S/C20H21FN4O2/c1-27-20-22-11-10-17(24-20)19-18(13-2-4-14(21)5-3-13)23-12-25(19)15-6-8-16(26)9-7-15/h2-5,10-12,15-16,26H,6-9H2,1H3/t15-,16-
| Molecular Formula | C20H21FN4O2 |
| Molecular Weight | 368.4047 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
SB239063 is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) alpha/beta inhibitor with IC50 of 44 nM, showing no activity against the gamma and delta kinase isoforms. SB 239063 is a potent inhibitor of inflammatory cytokine production, inhibits eosinophil recruitment, in addition to enhancing apoptosis of these cells and it can use for the treatment of asthma and other inflammatory disorders.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Lipid-soluble smoke particles upregulate vascular smooth muscle ETB receptors via activation of mitogen-activating protein kinases and NF-kappaB pathways. | 2008 Dec |
|
| A role of p38 mitogen-activated protein kinase in adenosine A₁ receptor-mediated synaptic depotentiation in area CA1 of the rat hippocampus. | 2008 Oct 23 |
|
| Bisphenol A-induced aromatase activation is mediated by cyclooxygenase-2 up-regulation in rat testicular Leydig cells. | 2010 Mar 15 |
|
| Aquaporin-4 in manganese-treated cultured astrocytes. | 2010 Sep |
|
| Human foetal intestinal fibroblasts are hyper-responsive to lipopolysaccharide stimulation. | 2012 Jan |
Patents
Sample Use Guides
Guinea Pig: SB 239063 (3, 10, or 30 mg/kg) was administered intragastrically via feeding tube 1 h before and 4 h after LPS challenge. For airway neutrophilia and IL-6 recovery experiments (48-h studies), SB 239063 was administered twice, 6 h apart, on the day after LPS challenge. For MMP-9 and IL-6 recovery experiments (6-h studies), SB 239063 (30 mg/kg) was administered 1 h before and 4 h after LPS challenge.
Rats: SB 239063 were administered orally, followed 60 min later by a challenge with LPS (3.0 mg/kg ip). For time-course studies, 15 mg/kg of SB 239063 were administered orally 1, 2, 3, or 4 h before LPS challenge.
Route of Administration:
Other
During the treatment with 20 μM and 100 μM SB239063 of hippocampal slice cultures, was observed significantly reduction of the levels of the pro-inflammatory cytokine IL-1beta and reduction of cell death after oxygen-glucose deprivation, in addition was seen strikingly diminishing of microglia activation
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 09:24:38 UTC 2023
by
admin
on
Sat Dec 16 09:24:38 UTC 2023
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| Record UNII |
HII3DC8CPI
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| Record Status |
Validated (UNII)
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| Record Version |
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HII3DC8CPI
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193551-21-2
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5166
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DTXSID90274455
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admin on Sat Dec 16 09:24:38 UTC 2023 , Edited by admin on Sat Dec 16 09:24:38 UTC 2023
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