SB 239063 |
| Catalog No.GC10054 |
A selective p38 MAPK inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 193551-21-2
Sample solution is provided at 25 µL, 10mM.
SB239063 is a potent and selective p38 MAPK inhibitor with an IC50 of 44 nM against p38α MAPK while exihibited no activity against the γ- and δ-kinase isoforms [1].
In vitro: 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[2].
In vivo: Oral administration of 3–30 mg/kg SB 239063 given twice a day dose-dependently inhibited airway neutrophil infiltration and interleukin (IL)-6 levels 48 h after lipopolysaccharide (LPS) inhalation [1]. In a bleomycin-induced pulmonary fibrosis model rats, SB 239063 treatment (2.4 or 4.8 mg/day via osmotic pump) significantly inhibited bleomycin-induced right ventricular hypertrophy (indicative of secondary pulmonary hypertension) and increased in lung hydroxyproline synthesis (indicative of collagen synthesis and fibrosis) (1). In conscious guinea pigs, administration of SB 239063 (10 or 30 mg/kg p.o.) showed approximately 50% inhibition of OA-induced pulmonary eosinophil influx, measured by BAL 24 h after antigen(1). Orally administration of SB 239063 (30 mg/kg) attenuated IL-6 bronchoalveolar lavage fluid concentrations (> 90% inhibition) and MMP-9 activity (64% inhibition) measured 6 h after LPS exposure. In guinea pig cultured alveolar macrophages, SB 239063 inhibited LPS-induced IL-6 production with IC50 of 362 nM. In lipopolysaccharide-stimulated human peripheral blood monocytes, SB 239063 inhibited IL-1 and TNF-α production with an IC50 of 0.12 and 0.35 μM, respectively(1).
References:
[1] Underwood D C, Osborn R R, Bochnowicz S, et al. SB 239063, a p38 MAPK inhibitor, reduces neutrophilia, inflammatory cytokines, MMP-9, and fibrosis in lung[J]. American Journal of Physiology-Lung Cellular and Molecular Physiology, 2000, 279(5): L895-L902.
[2] Strassburger M, Braun H, Reymann K G. Anti-inflammatory treatment with the p38 mitogen-activated protein kinase inhibitor SB239063 is neuroprotective, decreases the number of activated microglia and facilitates neurogenesis in oxygen–glucose-deprived hippocampal slice cultures[J]. European journal of pharmacology, 2008, 592(1): 55-61.
| Cell experiment [1]: | |
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Cell lines |
Human isolated whole blood |
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Preparation method |
The solubility of this compound in DMSO is > 18.4 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
0.01 ~ 10 μM; 4 hrs |
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Applications |
In lipopolysaccharide-stimulated human whole blood, SB 239063 concentration-dependently inhibited the production of a series of inflammatory cytokines including IL-1, TNF-α, IL-8 and IL-6, with the IC50 values ranging from 0.02 to 0.09 μM. In contrast, SB 239063 only showed weak inhibition of IL-1ra production, with the IC50 value of ~ 2 μM. |
| Animal experiment [1]: | |
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Animal models |
A Bleomycin-induced pulmonary fibrosis rat model |
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Dosage form |
2.4 or 4.8 mg/day via osmotic pump |
|
Applications |
In a Bleomycin-induced pulmonary fibrosis rat model, SB 239063 significantly inhibited Bleomycin-induced right ventricular hypertrophy (indicative of secondary pulmonary hypertension), and substantially attenuated Bleomycin-induced lung hydroxyproline synthesis (indicative of collagen synthesis and fibrosis). |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Underwood D C, Osborn R R, Bochnowicz S, et al. SB 239063, a p38 MAPK inhibitor, reduces neutrophilia, inflammatory cytokines, MMP-9, and fibrosis in lung[J]. American Journal of Physiology-Lung Cellular and Molecular Physiology, 2000, 279(5): L895-L902. | |
| Cas No. | 193551-21-2 | SDF | |
| Chemical Name | 4-(4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl)cyclohexanol | ||
| Canonical SMILES | COC1=NC=CC(C2=C(C3=CC=C(F)C=C3)N=CN2C4CCC(O)CC4)=N1 | ||
| Formula | C20H21FN4O2 | M.Wt | 368.4 |
| Solubility | ≥ 18.4 mg/mL in DMSO, ≥ 46.8 mg/mL in EtOH with ultrasonic and warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7144 mL | 13.5722 mL | 27.1444 mL |
| 5 mM | 0.5429 mL | 2.7144 mL | 5.4289 mL |
| 10 mM | 0.2714 mL | 1.3572 mL | 2.7144 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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