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TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1.
| Cell Experiment | |
|---|---|
| Cell lines | HMC-1 |
| Preparation method | In the first part of the study, qPCR was employed to evaluate the expression of inflammatory mediators in HMC-1 cells treated with EXs-CSU-R or EXs-CSU-S. In the second part of the study, qPCR was used to evaluate the effects of MAPK, TLR2, and TLR4 inhibitors on the production of inflammatory mediators in HMC-1 cells induced by EXs-CSU-S and EXs-CSU-R. The concentrations of tryptase-1, histamine, IL-6, TNF-α, VEGF, CXCL-1, CXCL-5, and CCl-2 in the supernatants of HMC-1 cells incubated with EXs-CSU-S and EXs-CSU-R as well as the concentrations of mediators in 40 μg EXs were measured using ELISA kits according to the manufacturer’s instructions. Mediator concentrations were expressed as relative values normalized to those of the control group. |
| Concentrations | 5 μM |
| Incubation time | 8 h |
| Animal Experiment | |
|---|---|
| Animal models | Adjuvant-induced arthritis (AA) rat model |
| Formulation | Saline |
| Dosages | 30 mg/kg |
| Administration | Orally |
| Molecular Weight | 399.51 |
| Formula | C24H21N3OS |
| CAS Number | 303162-79-0 |
| Solubility (25°C) | DMSO 70 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] D Falck, et al. Tandem mass spectrometry study of p38α kinase inhibitors and related substances
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