| CAS NO: | 193551-21-2 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 368.4 |
|---|---|
| Formula | C20H21FN4O2 |
| CAS No. | 193551-21-2 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 60 mg/mL (162.9 mM) |
| Water: <1 mg/mL | |
| Ethanol: 7 mg/mL warmed (19.0 mM) | |
| Other info | Chemical Name: (1r,4r)-4-(4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl)cyclohexanol InChi Key: ZQUSFAUAYSEREK-WKILWMFISA-N InChi Code: 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- SMILES Code: O[C@H]1CC[C@H](N2C(C3=NC(OC)=NC=C3)=C(C4=CC=C(F)C=C4)N=C2)CC1 |
| Synonyms | SB 239063; SB-239063; SB239063 |
| In Vitro | In vitro activity: SB 239063 potently inhibits IL-1 and TNF-α production in LPS-stimulated human peripheral blood monocytes with IC50 of 120 and 350 nM, respectively. In oxygen-glucose-deprived hippocampal slice cultures, SB239063 strikingly reduces the levels of the pro-inflammatory cytokine IL-1beta, causes cell death after oxygen-glucose deprivation and significantly diminishes microglia activation. In human corneal endothelial cell, SB 239063 inhibits TGF-β(2) and FGF-2-induced cell migration. Kinase Assay: SB 239063 is a potent and selective p38 MAPK inhibitor (IC50 = 44 nM for p38α). It displays> 220-fold selectivity over ERK, JNK1 and other kinases; and is ~ 3-fold more selective than SB 203580. Cell Assay: In oxygen-glucose-deprived hippocampal slice cultures, treatment with 20 μM and 100 μM SB239063 significantly reduced the levels of the pro-inflammatory cytokine IL-1β and reduced cell death after oxygen-glucose deprivation and strikingly diminished microglia activation. |
|---|---|
| In Vivo | In both guinea pigs and mice, SB 239063 (10 mg/kg, p.o.) reduces antigen-induced airway eosinophilia. In air- and ozone-exposed C57/BL6 and MKP-1(-/-) mice, SB239063 inhibits bronchial contraction. |
| Animal model | Guinea pigs |
| Formulation & Dosage | Dissolved in acidified 0.5% Tragacanth; 30 mg/kg; p.o. |
| References | J Pharmacol Exp Ther. 2000 Apr;293(1):281-8; Eur J Pharmacol. 2008 Sep 11;592(1-3):55-61. |
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