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TAK-715

Cat. No. M3048
TAK-715 Structure
Size Price Availability Quantity
5mg USD 95  USD95 In stock
10mg USD 120  USD120 In stock
50mg USD 370  USD370 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
Preparation method
Concentrations
Incubation time
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
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

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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