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TAK-715

Cat. No. M3048

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TAK-715 Structure
Size Price Availability Quantity
1mg USD 40 In stock
5mg USD 95 In stock
10mg USD 135 In stock
25mg USD 270 In stock
50mg USD 400 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
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
Chemical Information
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
References

[1] Akira Kaieda, et al. Structure-based design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine-based p38 MAP kinase inhibitors

[2] D Falck, et al. Tandem mass spectrometry study of p38α kinase inhibitors and related substances

[3] Rita Azevedo, et al. X-ray structure of p38α bound to TAK-715: comparison with three classic inhibitors

[4] Folkert Verkaar, et al. Inhibition of Wnt/β-catenin signaling by p38 MAP kinase inhibitors is explained by cross-reactivity with casein kinase Iδ/ɛ

[5] Seiji Miwatashi, et al. Novel inhibitor of p38 MAP kinase as an anti-TNF-alpha drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent

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  Catalog
Abmole Inhibitor Catalog




Keywords: TAK-715 supplier, p38 MAPK, inhibitors, activators

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