A potent, cell permeable inhibitor of p38 MAP kinase (IC50=44nM for recombinant purified human p38α). Inhibits IL-1 and TNF-α production in LPS-stimulated human peripheral blood monocytes (IC50=120nM and 350nM, respectively). Reported to protect against mild excitotoxic neuronal injury caused by NMDA and provides substantial protection against cell death induced by either oxygen glucose deprivation (OGD) or magnesium deprivation in cultured neurons. Also, reduces myocardial reperfusion injury via inhibition of endothelial adhesion molecule expression and blockade of polymorphonuclear (PMN) accumulation.
Product Details
| Alternative Name: | trans-1-(4-Hydroxycyclohexyl)-4-(fluorophenyl)-5-(2-methoxypyrimidin-4-yl) imidazole |
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| Formula: | C20H21FN4O2 |
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| MW: | 368.4 |
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| CAS: | 193551-21-2 |
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| Purity: | ≥97% (HPLC) |
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| Identity: | Identity determined by 1H-NMR. |
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| Appearance: | White to off-white solid. |
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| Solubility: | Soluble in DMSO, 100% ethanol or dichlormethane (may require slight warming). |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Handling: | Protect from light. Packaged under inert gas. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Apelin-13 protects neurovascular unit against ischemic injuries through the effects of vascular endothelial growth factor: C. Huang, et al.; Neuropeptides
60, 67 (2016),
Application(s): Investigating possible signal transduction pathways in rat MCAO model,
Abstract;
Activation of p38 MAPK by reactive oxygen species is essential in a rat model of stress-induced gastric mucosal injury: Y.T. Jia, et al.; J. Immunol.
179, 7808 (2007),
Abstract;
p38 MAPK inhibition reduces myocardial reperfusion injury via inhibition of endothelial adhesion molecule expression and blockade of PMN accumulation: F. Gao, et al.; Cardiovasc. Res.
53, 414 (2002),
Abstract;
Sustained activation of p38 mitogen-activated protein kinase contributes to the vascular response to injury: H. Ju, et al.; J. Pharmacol. Exp. Ther.
301, 15 (2002),
Abstract;
The selective p38 inhibitor SB-239063 protects primary neurons from mild to moderate excitotoxic injury: J.J. Legos, et al.; Eur. J. Pharmacol.
447, 37 (2002),
Abstract;
SB 239063, a second-generation p38 mitogen-activated protein kinase inhibitor, reduces brain injury and neurological deficits in cerebral focal ischemia: F.C. Barone, et al.; J. Pharmacol. Exp. Ther.
296, 312 (2001),
Abstract;
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SB-239063, a potent and selective inhibitor of p38 map kinase: preclinical pharmacokinetics and species-specific reversible isomerization: K.W. Ward, et al.; Pharm. Res.
18, 1336 (2001),
Abstract;
SB 239063, a potent p38 MAP kinase inhibitor, reduces inflammatory cytokine production, airways eosinophil infiltration, and persistence: D.C. Underwood, et al.; J. Pharmacol. Exp. Ther.
293, 281 (2000),
Abstract;
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