SB 242235 |
Catalog No.GC37595
One-Click Copy Product Info
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SB-242235 is a potent and selective p38 MAP kinase inhibitor, with an IC50 of 1.0 μM in primary human chondrocytes.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 193746-75-7
Sample solution is provided at 25 µL, 10mM.
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SB-242235 is a potent and selective p38 MAP kinase inhibitor, with an IC50 of 1.0 μM in primary human chondrocytes[1]. IC50: 1.0 μM (p38 MAPK, primary human chondrocytes)[1]
SB 242235 (0-10 μM) dose-dependently inhibits the activation of MAPKAP K2 with an IC50 of 1.0 μM in human chondrocytes stimulated with IL-1β[1].SB 242235 inhibits intracellular p38 activity, MAPKAP K2 was then isolated from these cells and assayed using HSP27 as a substrate[1]. Western Blot Analysis[1] Cell Line: Human chondrocytes
SB242235 (100 mg/kg; p.o.) abolishes MAP-KAPK-2 activity and HSP27 phosphorylation[2].SB242235 inhibits expression of the pro-inflammatory cytokines interleukin (IL)-6 and KC (murine IL-8) and COX-2[2].SB-242235 is demonstrated non-linear elimination kinetics that manifested as a decrease in clearance with increasing dose and apparent oral bioavailability > 100% at high oral doses in rat and monkey[3]. Animal Model: Female SKH-1 hairless mice (4-6 weeks)[2]
[1]. Badger, A.M., et al., Differential effects of SB 242235, a selective p38 mitogen-activated protein kinase inhibitor, on IL-1 treated bovine and human cartilage/chondrocyte cultures. Osteoarthritis Cartilage, 2000. 8(6): p. 434-43. [2]. Kim AL , et al. Role of p38 MAPK in UVB-induced inflammatory responses in the skin of SKH-1 hairless mice. J Invest Dermatol. 2005 Jun;124(6):1318-25. [3]. Ward, K.W., et al., SB-242235, a selective inhibitor of p38 mitogen-activated protein kinase. I: preclinical pharmacokinetics. Xenobiotica, 2002. 32(3): p. 221-33.
| Cas No. | 193746-75-7 | SDF | |
| Canonical SMILES | COC1=NC=CC(C2=C(C3=CC=C(F)C=C3)N=CN2C4CCNCC4)=N1 | ||
| Formula | C19H20FN5O | M.Wt | 353.39 |
| Solubility | DMSO: ≥ 48 mg/mL (135.83 mM) | 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 | 2.8297 mL | 14.1487 mL | 28.2973 mL |
| 5 mM | 565.9 μL | 2.8297 mL | 5.6595 mL |
| 10 mM | 283 μL | 1.4149 mL | 2.8297 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 saline, 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: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)