| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
Purity: ≥98%
SB-242235 has the potential to treat cytokine-mediated illnesses like autoimmune or inflammatory diseases because it is a potent and selective p38 MAP kinase inhibitor with an IC50 of 1.0 uM. Positive pharmacokinetic results were seen with SB-242235. However, SB-242235 showed low to moderate clearance with plasma half-lives > 4 hours in non-rodent species. Systemic plasma clearance was high in rats. The oral bioavailability was high in all preclinical species. With increasing dose, SB-242235's clearance decreased in rats and monkeys, and at high oral doses, its apparent oral bioavailability appeared to be > 100%. These non-linear elimination kinetics were also evident in the drug's apparent oral bioavailability.
| Targets |
p38 MAPK (IC50 = 1.0 μM)
|
|---|---|
| ln Vitro |
SB 242235 (0-10 μM) inhibits MAPKAP K2 activation in a dose-dependent manner 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 assessed using HSP27 as a substrate[1].
|
| ln Vivo |
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]. In rats and monkeys, SB-242235 has been shown to have non-linear elimination kinetics, which showed up as a decrease in clearance with dose and an apparent oral bioavailability > 100% at high oral doses[3]. |
| Enzyme Assay |
SB 242235 inhibited intracellular p38 activity, human chondrocytes were treated with different doses of SB 242235 prior to stimulation with IL-1_ for 15 min. From these cells, MAPKAP K2 was then isolated and measured using HSP27 as a substrate. With an IC50 of 1.0 uM, SB 242235 inhibited the activation of MAPKAP K2 in a dose-dependent manner.
|
| Animal Protocol |
Female SKH-1 hairless mice (4–6 weeks)[2]
100 mg/kg Oral administered, 30 minutes prior to ultraviolet B (UVB) irradiation |
| References |
|
| Molecular Formula |
C18H17N5O3
|
|
|---|---|---|
| Molecular Weight |
351.36
|
|
| Exact Mass |
351.13
|
|
| Elemental Analysis |
C, 61.53; H, 4.88; N, 19.93; O, 13.66
|
|
| CAS # |
193746-75-7
|
|
| Related CAS # |
|
|
| Appearance |
white solid powder
|
|
| SMILES |
COC1=NC=CC(=N1)C2=C(N=CN2C3CCNCC3)C4=CC=C(C=C4)F
|
|
| InChi Key |
PDTYLGXVBIWRIM-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C19H20FN5O/c1-26-19-22-11-8-16(24-19)18-17(13-2-4-14(20)5-3-13)23-12-25(18)15-6-9-21-10-7-15/h2-5,8,11-12,15,21H,6-7,9-10H2,1H3
|
|
| Chemical Name |
4-[5-(4-fluorophenyl)-3-piperidin-4-ylimidazol-4-yl]-2-methoxypyrimidine
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.07 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8461 mL | 14.2304 mL | 28.4608 mL | |
| 5 mM | 0.5692 mL | 2.8461 mL | 5.6922 mL | |
| 10 mM | 0.2846 mL | 1.4230 mL | 2.8461 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
